bluuebunny/crossref_metadata_2025_split huggingface dataset:
Bioactive Natural Products from Papua New Guinea Marine Sponges
Authors: Noro Jeffery C. , Kalaitzis John A. , Neilan Brett A. 
Published: October 2012

AbstractThe discovery of novel natural products for drug development relies heavily upon a rich biodiversity, of which the marine environment is an obvious example. Marine natural product research has spawned several drugs and many other candidates, some of which are the focus of current clinical trials. The sponge megadiversity of Papua New Guinea is a rich but underexplored source of bioactive natural products. Here, we review some of the many natural products derived from PNG sponges with an emphasis on those with interesting biological activity and, therefore, drug potential. Many bioactive natural products discussed here appear to be derived from non‐ribosomal peptide and polyketide biosynthesis pathways, strongly suggesting a microbial origin of these compounds. With this in mind, we also explore the notion of sponge‐symbiont biosynthesis of these bioactive compounds and present examples to support the working hypothesis.
Cytotoxic Tetraprenylated Alkaloids from the South China Sea Gorgonian Euplexaura robusta
Authors: Zhang Jin‐Rong , Li Ping‐Lin , Tang Xu‐Li , Qi Xin , Li Guo‐Qiang 
Published: October 2012

AbstractNine achiral tetraprenylated alkaloids, including three new compounds, named malonganenones I–K (1–3, resp.), together with six known analogs, 4–9, were isolated from the gorgonian Euplexaura robusta collected from Weizhou Island of Guangxi Province, China. The structures of compounds 1–3 were elucidated by extensive spectral analyses, especially of their 1D‐ and 2D‐NMR data. Compounds 1, 4, 6, and 7 showed moderate cytotoxicities against K562 and HeLa tumor cell lines with IC50 values ranging from 0.35 to 10.82 μM. Compound 6 also showed moderate inhibitory activity against c‐Met kinase at a concentration of 10 μM.
Chemical Diversity of Wild Growing Origanum majorana in Cyprus
Authors: Karousou Regina , Efstathiou Chrysa , Lazari Diamanto 
Published: October 2012

AbstractThe present work aims at tracing the essential‐oil diversity of wild growing Origanum majorana plants in Cyprus. The study of six populations scattered over the western part of the island has shown that the essential oils were rich either in trans‐sabinene hydrate/terpinen‐4‐ol or in α‐terpineol/trans‐sabinene hydrate. The former oil type is more common and responsible for the typical marjoram odor of the plants. The comparison of our results with published data concerning wild and cultivated O. majorana showed that the oil composition of the Cypriot populations had not been reported from wild plants from other parts of the Mediterranean region, while it is very common among the cultivated plants. Thus, it seems probable that the nowadays cultivated marjoram may originate from Cypriot wild populations.
Sulfur‐Containing Ferrocenyl Alcohols and Oximes: New Promising Antistaphylococcal Agents
Authors: Ilić Danijela , Damljanović Ivan , Stevanović Dragana , Vukićević Mirjana , Blagojević Polina , Radulović Niko , Vukićević Rastko D. 
Published: October 2012

AbstractA small library containing four different series of new ferrocene derivatives, 2‐(alkylsulfanyl)‐1‐ferrocenylethan‐1‐ols, 3‐(alkylsulfanyl)‐1‐ferrocenylpropan‐1‐ols, (E)‐ and (Z)‐2‐(alkylsulfanyl)‐1‐ferrocenylethan‐1‐one oximes, and (E)‐ and (Z)‐3‐(alkylsulfanyl)‐1‐ferrocenylpropan‐1‐one oximes (36 different compounds in total) was synthesized starting from ferrocene and the corresponding sulfanyl acids. All compounds were spectrally (IR and NMR) and electrochemically characterized. In general, the obtained compounds were found to exhibit very strong antimicrobial activities (broth microdilution assay) against the tested microorganisms (six common human pathogens). For the majority of the tested compounds, the determined MIC values were either under the 10 μg/ml MIC limit recognized to delimit efficient antimicrobials or were comparable to/lower than those of the used positive controls (tetracycline/nystatin). The most susceptible organism was found to be Staphylococcus aureus with MIC values even reaching 0.001 μg/ml. The presence of CH(OH)(CH2)nS and CH(NOH)(CH2)nS (n=1 or 2) structural fragments seems to be essential for the observed strong activity (introduction of hydroxyimino and alcohol functionalities, instead of the keto function, resulted in a more than 105‐fold increase in antistaphylococcal activity in some instances). Nevertheless, a possible influence of the ferrocenyl‐core redox chemistry (Fe2+/Fe3+) should not be disregarded. The studied alcohols exhibited a reversible one‐electron redox couple at almost the same position as ferrocene, while the hydroxyimino group conjugated with cyclopentadienyl ring considerably shifted the redox potential of the ferrocene unit in oximes.
Variation in Terpene and Linear‐Chain Hydrocarbon Content in Yarrow (Achillea millefolium L.) Germplasm from the Rhaetian Alps, Italy
Authors: Pecetti Luciano , Tava Aldo , Romani Massimo , Cecotti Roberto , Mella Mariella 
Published: October 2012

AbstractYarrow (Achillea millefolium L.) is a herbaceous species common in the Alpine region of Europe and used in folk medicine since antiquity. Its organs are rich in monoterpenes and sesquiterpenes, two subclasses of plant terpenoids with relevant ecological significance, which were reported as valuable markers for the traceability of mountain dairy products. The variability in chemical composition of yarrow germplasm may be related with its genetic diversity, accounting for possible differences in medical properties, and supporting its use as a specific territorial marker. Aim of this work was to assess the leaf chemical composition of 16 yarrow populations collected at altitudes exceeding 1600 m in three valleys of the Rhaetian Alps, Italy, and jointly evaluated in a lowland site. The most abundant compounds detected generally differed from those of the germplasm from other countries. A trend of valley‐specific pattern of composition was evident. However, the variability among individual populations was even more remarkable, regardless of their valley of origin. The concentrations of sesquiterpene hydrocarbons, oxygenated monoterpenes, and oxygenated sesquiterpenes discriminated the populations in multivariate analysis. A few prevailing chemotypes were characterized, which differed from those previously reported in the literature. The geographic isolation from other germplasms, and the local ecotypization, likely originated a chemically distinct gene pool.
Studies on Chemical‐Structure Modification and StructureActivity Relationship of Gambogic Acid Derivatives at Carbon(34)
Authors: Zhang Xiao‐Jin , Li Xiang , Yang Ying‐Rui , Sun Hao‐Peng , Gao Yuan , Zhang Lei , Wang Jin‐Xin , Guo Qing‐Long , You Qi‐Dong 
Published: October 2012

AbstractGambogic acid (GA), a natural product, was identified as a promising antitumor agent. To further explore the structureactivity relationship of GA and discover novel GA derivatives as antitumor agents, 19 novel GA derivatives modified at C(34) were synthesized and evaluated against A549, BGC‐823, U251, HepG2, and MB‐231 cancer cell lines by cellular assays. Among them, 15 compounds were found to be more potent than GA against some cancer cell lines. Notably, compound 3 possessed potent inhibitory activities against five cell lines with IC50 values ranging between 0.24 and 1.09 μM. Compounds 9 and 18 were seven to eightfold more active than GA against A549 cell line. Chemical modification at C(34) of GA by introducing of hydrophilic aliphatic amines resulted in increased activity and improved drug‐like properties. These findings will enhance our understanding of the SAR of GA and can lead to the discovery of novel GA derivatives as potential antitumor agents.
Synthesis, and in vitro Enzymatic and Antiviral Evaluation of d4T Polyphosphate Derivatives as Chain Terminators
Authors: Yang Shiqiong , Pannecouque Christophe , Herdewijn Piet 
Published: October 2012

AbstractA series of d4T di‐ or triphosphate derivatives have been synthesized and evaluated as effective substrates for HIV‐1 RT, and also tested for their in vitro anti‐HIV activity. The steady‐state kinetic study of compounds 1–4 in an enzymatic incorporation assay by HIV‐1 RT follows MichaelisMenten profile. In addition, compounds 2–4 are able to inhibit HIV‐1 replication to the same extent as d4T and d4TMP in MT‐4 cells, as well as in CEM/0 cells and CEM/TK− cells. The data suggests that these d4T polyphosphate derivatives are hydrolyzed to d4T and rephosphorylated to d4TTP before exerting their antiviral activity.
Doing the Right Thing: Ethical Leadership and Decision Making
Authors: Garza Mitchell Regina L. 
Published: October 2012

AbstractThis chapter explores the relationship between leadership style, ethical orientation, and the AACC competencies. A glimpse of the competencies in practices is provided through the results of interviews with thirteen community college presidents. The findings presented here are culled from a larger study of presidential decision making during difficult times (Garza Mitchell and Hornak, 2010; Hornak and Garza Mitchell, 2010) that was funded by a Faculty Research and Creative Endeavors grant from Central Michigan University.
A Highly Stereoselective Synthesis of Glycidic Amides Based on a New Class of Chiral Sulfonium Salts: Applications in Asymmetric Synthesis
Authors: Sarabia Francisco , Vivar‐García Carlos , García‐Castro Miguel , García‐Ruiz Cristina , Martín‐Gálvez Francisca , Sánchez‐Ruiz Antonio , Chammaa Samy 
Published: October 2012

AbstractA new type of chiral sulfonium salts that are characterized by a bicyclic system has been designed and synthesized from α‐amino acids. Their corresponding ylides, which were prepared by basic treatment of the sulfonium salts, reacted smoothly with a broad array of simple and chiral aldehydes to provide trans‐epoxy amides in reasonable to very good yields and excellent stereoselectivities (>98 %). The obtained epoxy amides were found to be useful as synthetic building blocks. Thus, they were reduced into their corresponding epoxy alcohols and subjected to oxirane‐ring‐opening reactions with different types of nucleophiles.
Eco‐Friendly Combination of the Immobilized PGA Enzyme and the S‐Phacm Protecting Group for the Synthesis of Cys‐Containing Peptides
Authors: Góngora‐Benítez Miriam , Basso Alessandra , Bruckdorfer Thomas , Royo Miriam , Tulla‐Puche Judit , Albericio Fernando 
Published: October 2012

AbstractEnzyme‐labile protecting groups have emerged as a green alternative to conventional protecting groups. These groups introduce a further orthogonal dimension and eco‐friendliness into protection schemes for the synthesis of complex polyfunctional organic molecules. S‐Phacm, a Cys‐protecting group, can be easily removed by the action of a covalently immobilized PGA enzyme under very mild conditions. Herein, the versatility and reliability of an eco‐friendly combination of the immobilized PGA enzyme and the S‐Phacm protecting group has been evaluated for the synthesis of diverse Cys‐containing peptides.
Cyclohexyne Cycloinsertion in the Divergent Synthesis of Guanacastepenes
Authors: Gampe Christian M. , Carreira Erick M. 
Published: October 2012

AbstractThe guanacastepenes are a family of 15 diterpenes that share a common 5‐6‐7 tricyclic core, which is decorated with quaternary centers, unsaturation, hydroxyl and carbonyl groups. Some of these natural products show interesting antimicrobial potency. Their collective structural and biological features have stirred up vibrant activity among organic chemists. Herein, we disclose an account of our studies toward the synthesis of a number of guanacastepenes. The synthetic strategy relies on the use of cyclohexyne in a cycloinsertion reaction to rapidly construct the guanacastepene core. Isolation of a cyclobutenol as intermediate in the cyclohexyne cycloinsertion provided us with the possibility to study further the reactivity of this metastable compound, and we uncovered novel rearrangements and ring‐opening reactions. Stereoselective, late‐stage oxidative diversification of the carbon scaffold allowed the synthesis of guanacastepenes N and O and paved the way for the synthesis of guanacastepenes H and D.
ChemInform Abstract: Hydrolysis Studies on Bismuth Nitrate: Synthesis and Crystallization of Four Novel Polynuclear Basic Bismuth Nitrates.
Authors: Miersch L. , Rueffer T. , Schlesinger M. , Lang H. , Mehring M. 
Published: October 2012

AbstractThe structures of (II)—(V) are determined by single crystal XRD.
ChemInform Abstract: Synthesis, Structure, and Characterization of New Li+—d0—Lone‐Pair — Oxides: Noncentrosymmetric Polar Li6(Mo2O5)3 (SeO3)6 and Centrosymmetric Li2(MO3)(TeO3) (M: Mo6+ or W6+).
Authors: Nguyen Sau Doan , Halasyamani P. Shiv 
Published: October 2012

AbstractCompounds (III) and (VII) are characterized by single crystal XRD, IR and UV/VIS diffuse reflectance spectroscopy, second harmonic generation, piezoelectric, and polarization measurements, and electron localization function computations using the plane‐wave pseudopotential method.
ChemInform Abstract: Convenient Method for Reduction of C—N Double Bonds in Oximes, Imines, and Hydrazones Using Sodium Borohydride—Raney Ni System.
Authors: Yang Yihua , Liu Shouxin , Li Junzhang , Tian Xia , Zhen Xiaoli , Han Jianrong 
Published: October 2012

AbstractAn efficient method for the reduction of C—N double bonds is successfully applied to a wide range of oximes, imines and hydrazones.
ChemInform Abstract: Chlorination of Aliphatic Primary Alcohols via Triphosgene—Triethylamine Activation.
Authors: Ayala Caitlan E. , Villalpando Andres , Nguyen Alex L. , McCandless Gregory T. , Kartika Rendy 
Published: October 2012

AbstractDiols bearing a primary and a tertiary hydroxyl group such as (Ia) and (Ib) are selectively chlorinated at the primary function.
ChemInform Abstract: Ni(0)/NHC‐Catalyzed Amination of N‐Heteroaryl Methyl Ethers Through the Cleavage of Carbon—Oxygen Bonds.
Authors: Tobisu Mamoru , Yasutome Ayaka , Yamakawa Ken , Shimasaki Toshiaki , Chatani Naoto 
Published: October 2012

AbstractOptimized conditions are developed for the conversion of electron‐deficient substrates to the corresponding amino‐substituted derivatives.
ChemInform Abstract: Oxidative Imination of Toluenes Catalyzed by Pd—Au/Silica Gel under Mild Reaction Conditions.
Authors: Cui Xinjiang , Shi Feng , Deng Youquan 
Published: October 2012

AbstractA heterogenous bimetallic catalyst is prepared and successfully applied for the oxidative imination of toluenes with amines (I) and sulfonamides (IV).
ChemInform Abstract: Polystyrene‐Supported Pyridinium Chloroaluminate Ionic Liquid as a New Heterogeneous Lewis Acid Catalyst for Knoevenagel Condensation.
Authors: Boroujeni Kaveh Parvanak , Jafarinasab Mina 
Published: October 2012

AbstractThe catalyst is synthesized from commercially available Merrifield resin, pyridine and AlCl3 and successfully applied in the Knoevenagel condensation of aromatic and aliphatic aldehydes with ethyl cyanoacetate (I) as well as in the Michael reaction of hydroxycoumarin (X) with benzaldehyde.
ChemInform Abstract: Highly Efficient Solvent‐Free Acetylation of Alcohols with Acetic Anhydride Catalyzed by Recyclable Sulfonic Acid Catalyst (SBA‐15‐Ph—Pr—SO3H) — An Environmentally Benign Method.
Authors: Zareyee Daryoush , Ghadikolaee Abdollah Razaghi , Khalilzadeh Mohammad A. 
Published: October 2012

AbstractA highly thermal stable, hydrophobic, reusable (5 times), easily preparable, and complete heterogeneous catalyst, which can also be stored and handled under open air , is successfully applied to the title reaction.
ChemInform Abstract: Synthesis of gem‐Dihaloenynes and Butatrienes from gem‐Dihalovinyl Derivatives.
Authors: Meng Tianhao , Zhang Hui‐Jun , Xi Zhenfeng 
Published: October 2012

AbstractA BuLi‐mediated Fritsch—Buttenberg—Wiechell rearrangement of tetrahalobutadienes gives the gem‐dihaloenyne products in good yields.
ChemInform Abstract: An Efficient Synthesis of Tertiary Amines from Nitriles in Aprotic Solvents.
Authors: Shares Jonathan , Yehl Jenna , Kowalsick Amanda , Byers Philip , Haaf Michael P. 
Published: October 2012

AbstractThe process affords the desired amines, required as non‐nucleophilic proton scavengers, exclusively from nitriles (I) in THF, hexanes or pentane.
ChemInform Abstract: A Robust, Efficient, and Highly Enantioselective Method for Synthesis of Homopropargyl Amines.
Authors: Vieira Erika M. , Haeffner Fredrik , Snapper Marc L. , Hoveyda Amir H. 
Published: October 2012

AbstractThe first general, practical, scalable, and efficient method for the synthesis of the title compounds is developed by using an inexpensive metal salt and a readily preparable ligand (five steps).
ChemInform Abstract: N,N‐Dichlorotriflamide in the Reaction with Cinnamic Acid.
Authors: Kondrashov E. V. , Popov A. V. , Chernyshev K. A. , Serykh V. Yu. , Rozentsveig I. B. 
Published: October 2012

AbstractAn uncommon chloroamidation of cinnamic acid accompanied by a decarboxylation is observed on reacting cinnamic acid with triflamide (II) in water in the absence of any catalyst.
ChemInform Abstract: Efficient Microwave‐Assisted Pd‐Catalyzed Hydroxylation of Aryl Chlorides in the Presence of Carbonate.
Authors: Yu Chao‐Wu , Chen Grace S. , Huang Chen‐Wei , Chern Ji‐Wang 
Published: October 2012

AbstractUsing a weak base carbonate, even the hydroxylation of chlorides bearing an ester (IIe) or a free amide (IIf) group succeeds without hydrolysis.
ChemInform Abstract: Combination of NH2OH·HCl and NaIO4: A New and Mild Oxidizing Agent for Selective Oxidation of Alcohols to Carbonyl Compounds.
Authors: Majee Adinath , Kundu Shrishnu Kumar , Santra Sougata , Hajra Alakananda 
Published: October 2012

AbstractThe optimized process is advantageous with regard to simple operation, fast reaction, and neutral conditions.
ChemInform Abstract: Oxofunctionalized trans‐2‐Carboxycinnamic Acids by Catalytic Domino Oxidation of Naphthols and Hydronaphthoquinones.
Authors: Giurg Miroslaw , Muchalski Hubert , Kowal Ewa 
Published: October 2012

AbstractBoth β‐ (I) and α‐naphthols (III) are converted to carboxycinnamic acids (II) by hydrogen peroxide oxidation in the presence of a diaryl diselenide.
ChemInform Abstract: Nitromethyl Benzoate Annulation Reactions: A Rapid Construction of the Stealthin Skeleton.
Authors: Kraus George A. , Chaudhary Divya , Yuan Yi , Schuster Andrew 
Published: October 2012

AbstractA Michael addition/Claisen condensation sequence affords polycyclic adducts representing the carbocyclic framework of stealthins.
ChemInform Abstract: Synthesis and Characterization of Novel Ionic Liquids: N‐Substituted Aziridinium Salts.
Authors: Duriska Martin B. , Grondin Joseph , Servant Laurent , Birot Marc , Deleuze Herve 
Published: October 2012

AbstractSome representative compounds of a new family of room‐temperature ionic liquids built from aziridinium cations are prepared.
ChemInform Abstract: Synthesis of Certain 2‐Substituted‐1H‐benzimidazole Derivatives as Antimicrobial and Cytotoxic Agents.
Authors: Taher Azza Taher , Khalil Nadia Abdalla , Ahmed Eman Mohamed , Ragab Yasser Mohamed 
Published: October 2012

AbstractAll new benzimidazole derivatives show potent antimicrobial activities against some species of Gram‐negative bacteria (P.
ChemInform Abstract: Substituted [1,3,4]‐Oxadiazole, [1,3,4]‐Thiadiazole and [1,2,4]‐Triazole; Synthesis, Characterization and Antimicrobial Study.
Authors: Deohate Pradip P. 
Published: October 2012

AbstractA variety of benzotriazolylmethyl‐substituted oxadiazole, thiadiazole and triazole derivatives are synthesized via oxidative cyclization reactions of acetamidothiourea derivatives (III).
ChemInform Abstract: “Click” Synthesis of a Triazole‐Based Inhibitor of Met Functions in Cancer Cells.
Authors: Passarella Daniele , et al. et al. 
Published: October 2012

AbstractCompound (I) inhibits the HGF‐induced scattering of MDCK (epithelial cells) and in vitro tumorigenesis of H1437 (non‐small‐cell lung cancer) and GTL‐16 (human gastric carcinoma).
ChemInform Abstract: Phosphomolybdic Acid (H3Mo12O40P) as a Reusable Heterogeneous Catalyst for the Synthesis of 5‐Substituted 1H‐Tetrazoles via [2 + 3] Cycloaddition of Nitriles and Sodium Azide.
Authors: Takale Santosh , Manave Smita , Phatangare Kiran , Padalkar Vikas , Darvatkar Nitin , Chaskar Atul 
Published: October 2012

AbstractThe applied catalyst can be reused several times.
ChemInform Abstract: Asymmetric Friedel—Crafts Alkylation of Indoles with 3‐Nitro‐2H‐chromenes Catalyzed by Diphenylamine‐Linked Bis(oxazoline) and Bis(thiazoline) Zn(II) Complexes.
Authors: Jia Yang , Yang Wen , Du Da‐Ming 
Published: October 2012

AbstractThe mild and efficient title reaction leads to medicinally privileged indolyl(nitro)chromans.
ChemInform Abstract: An Efficient Intermolecular [Pd]‐Catalyzed C—C and Intramolecular [Cu]‐Catalyzed C—O Bonds Formation: Synthesis of Functionalized Flavans and Benzoxepine.
Authors: Suchand B. , Krishna J. , Ramulu B. Venkat , Dibyendu D. , Reddy A. Gopi Krishna , Mahendar L. , Satyanarayana G. 
Published: October 2012

AbstractA three step synthesis of flavans is based on the copper catalyzed cyclization of propanol derivatives (V) and (VII).
ChemInform Abstract: Potassium Phosphate Catalyzed Efficient Synthesis of 3‐Carboxycoumarins.
Authors: Undale Kedar A. , Gaikwad Dipak S. , Shaikh Tarannum S. , Desai Uday V. , Pore Dattaprasad M. 
Published: October 2012

AbstractAn efficient and fast synthesis of the title compounds (III) (11 examples) is achieved by reaction of salicylaldehyde (I) with Meldrum′s acid using potassium phosphate as an inexpensive catalyst.
ChemInform Abstract: Enantioselective Friedel—Crafts Alkylation of Indoles with 2‐Enoylpyridine‐N‐oxides Catalyzed by glucoBOX‐Cu(II) Complex.
Authors: George Jimil , Reddy B. V. Subba 
Published: October 2012

AbstractThe use of sugar‐based chiral ligands renders possible a highly efficient reaction in a short reaction time.
ChemInform Abstract: An Efficient Synthesis of 2‐Alkylpyridines Using an Alkylation/Double Decarboxylation Strategy.
Authors: Donald Craig , Boyd Scott 
Published: October 2012

AbstractA convenient method is presented for the synthesis of 2‐alkylpyridines from pyridyl malonate ester (I) via alkylation with alkyl bromides and subsequent hydrolysis and double decarboxylation.
ChemInform Abstract: Synthesis of Novel 6‐Substituted Sulfur‐Containing Derivatives of Pyridoxine.
Authors: Shtyrlin Nikita V. , Pavelyev Roman S. , Pugachev Mikhail V. , Sysoeva Lubov P. , Musin Rashid Z. , Shtyrlin Yurii G. 
Published: October 2012

AbstractDerivatives bearing 1,2 or 3 chloro substituents are prepared and used as starting materials for different types of title compounds.
ChemInform Abstract: Chiral Counteranion‐Directed Silver‐Catalyzed Asymmetric Synthesis of 1,2‐Dihydroisoquinolines by Friedel—Crafts Alkylation Reactions.
Authors: Zhang Jun‐Wei , Xu Zhe , Gu Qing , Shi Xiao‐Xin , Leng Xue‐Bing , You Shu‐Li 
Published: October 2012

AbstractBest results are obtained with the binol‐derived silver phosphate BSP in the reaction of o‐alkynyl‐substituted aldimines with indoles.
ChemInform Abstract: Discovery, Oral Pharmacokinetics and in vivo Efficacy of a Highly Selective 5‐HT4 Receptor Agonist: Clinical Compound TD‐2749.
Authors: Long Daniel D. , et al. et al. 
Published: October 2012

AbstractApplication of the previously reported multivalent approach to drug discovery towards 5‐HT4 receptor agonists results in the identification of (I), which is selected as a development candidate.
ChemInform Abstract: Hydrothiolation and Intramolecular Cyclization Sequence for the Synthesis of 1,3‐Oxathiine Frameworks.
Authors: Nishina Yuta , Miyata Junya 
Published: October 2012

AbstractStarting from thiosalicylic acid, unactivated alkynes in the presence of a Pd‐catalyst and activated alkynes in the absence of the catalyst are selectively transformed to the desired heterocycles without any by‐products.