Patent ID: 9156793
Filing Date: 2015-10-13
Classification: C07D

Abstract:
1. A method for the preparation of a compound of formula (XX): the method comprises four steps, the four steps are a step (Q1), a step (Q2), a step (N) and a step (M1); compound of formula (XX) is prepared in step (M1); step (M1) comprises a reaction (M1-reac); reaction (M1-reac) is a reaction between a compound of formula (XXI), a reagent (M-reag) and a reagent (M-A) in a solvent (M-solv); reagent (M-reag) is selected from the group consisting of p-toluenesulfonylmethyl isocyanide, trifluoromethanesulfonylmethyl isocyanide, methanesulfonylmethyl isocyanide, benzenesulfonylmethyl isocyanide, and 4-acetamidobenzenesulfonylmethyl isocyanide, or mixtures thereof; reagent (M-A) is selected from the group consisting of ammonia, sulfamic acid, p-toluenesulfonamide, benzenesulfonamide, 4-acetamidobenzenesulfonamide, tritylamine, formamide, urea, urotropine, ethyl carbamate, and acetamide, or mixtures thereof; solvent (M-solv) is selected from the group consisting of N,N-dimethylformamide, C compound of formula (XX) is prepared in step (N); step (N) comprises a reaction (N-reac); reaction (N-reac) is a reaction of a compound of formula (XXII) with a catalyst (N-cat); catalyst (N-cat) is selected from the group consisting of acetic acid, formic acid, trifluoroacetic acid, methanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, camphorsulfonic acid HCl, HBr, H step (Q1) comprises a reaction (Q1-reac); reaction (Q1-reac) is a reaction of compound of formula (XXV) with a reagent (Q1-read) to provide a reaction product of reaction (Q1-reac); R1 is Br, Cl, or I; reagent (Q1-reag) is selected from the group consisting of lithium, magnesium, aluminum, zinc, calcium, propylmagnesium chloride, propylmagnesium bromide, and butyllithium, or mixtures thereof; step (Q2) comprises a reaction (Q2-reac); reaction (Q2-reac) is a reaction of the reaction product of reaction (Q1-reac) with chloroacetone; compound of formula (XXII) is prepared by the reaction (Q2-reac).