Patent ID: 7091360

Claim:
A process of preparing a reagent of formula (Ia): comprising reacting a compound of formula (I): wherein: X is —O— or —S—; Y is nitrogen or —CR 3a —; Y′ is nitrogen or —CR 2a — provided that Y and Y′ are not simultaneously nitrogen; one of R 2 and R 3 is hydrogen, (C 1-6 )alkyl, (C 1-6 )alkoxy, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 1-6 )alkylthio, (C 5-6 )cycloalkyl, (C 5-6 )cycloalkylalkyl, halo, nitro, halo(C 1-3 )alkyl, (C 6-12 )aryl, heteroaryl, heterocycloalkyl, (C 6-12 )aryl(C 1-6 )alkyl, heteroaryl(C 1-6 )alkyl, (C 1-6 )alkylsulfonyl, (C 6-12 )arylsulfonyl, (C 6-12 )aryl(C 1-6 )alkylsulfonyl, heteroarylsulfonyl, heteroaryl(C 1-6 )-alkylsulfonyl, aminosulfonyl, (C 1-6 )alkylaminosulfonyl, (C 1-6 )dialkylaminosulfonyl, —CONR 4 R 5 (where R 4 and R 5 are independently of each other hydrogen, (C 1-6 )alkyl, (C 1-6 )alkoxy, aryl, aryl(C 1-6 )alkyl, heteroaryl, heteroaryl(C 1-6 )alkyl, (C 5-6 )cycloalkyl, (C 5-6 )cycloalkyl(C 1-6 )alkyl, heterocycloalkyl, or heterocycloalkyl(C 1-6 )alkyl, or R 4 and R 5 together with the nitrogen atom to which they are attached form heterocycloamino), —NHCOR 6 (where R 6 is (C 1-6 )alkyl, (C 6-12 )aryl, aryl(C 1-6 )alkyl, heteroaryl, heteroaryl(C 1-6 )alkyl, (C 5-6 )cycloalkyl, (C 5-6 )cycloalkyl(C 1-6 )alkyl, heterocycloalkyl, or heterocycloalkyl(C 1-6 )alkyl), —SO 2 NR 7 R 8 (where R 7 and R 8 are independently of each other hydrogen, (C 1-6 )alkyl, (C 6-12 )aryl, (C 6-12 )aryl(C 1-6 )alkyl, heteroaryl, heteroarylalkyl, (C 5-6 )cycloalkyl, (C 5-6 )cycloalkyl(C 1-6 )alkyl, heterocycloalkyl, or heterocycloalkyl(C 1-6 )alkyl, or R 7 and R 8 together with the nitrogen atom to which they are attached form heterocycloamino), -alkylene-CONR 4 R 5 (where R 4 and R 5 are as defined above), —alkylene-NHCOR 6 (where R 6 is as defined above), or -alkylene-SO 2 NR 7 R 8 (where R 7 and R 8 are as defined above); and the other of R 2 and R 3 is hydrogen or (C 1-6 )alkyl wherein within R 2 or R 3 said aryl, heteroaryl, or heterocycloalkyl is optionally substituted further with one, two, or three substituents independently selected from the group consisting of (C 1-6 )alkoxy, (C 1-6 )alkyl, (C 6-12 )aryl(C 1-6 )alkyl, halo, nitro, and halo(C 1-3 )alkyl; or when Y and Y′ are carbon, then R 2 and R 3 together with the atoms to which they are attached form an optionally substituted benzene, napthyl, (C 3-6 )cycloalkyl, or an aromatic or non-aromatic heterocyclic ring; R 2a and R 3a are independently hydrogen or alkyl; or R 2a and R 3a together form a covalent bond, provided that when Y or Y′ is nitrogen, R 2a and R 3 or R 2 and R 3a together form a covalent bond; with a Grignard reagent wherein Z is a halogen provided that (I) is not 1,2,4- or 1,3,4-oxadiazole.