Processes for the synthesis of 2-amino-4,6-dimethoxybenzamide and other benzamide compounds

摘要

This invention provides a method for the synthesis of a 2-amino-4,6-dimethoxybenzamide and other benzamides of Compound I: wherein R1, R2, R3, and R4 each independently represent a hydrogen, a C1-C6 alkyl, or a C1-C6 alkoxy; and wherein R6 and R7 each independently represent a hydrogen, a C1-C6 alkyl, a protecting group, or a directing group.;

主权项

1. A process for producing at least one wherein the process comprises: (i) combining at least one with at least one halogenating agent to produce at least one (ii) combining the at least one Compound III with at least one cyanating agent to produce at least one and; (iii) combining the at least one Compound IV with at least one hydrating agent and/or at least one hydrating catalyst to produce the at least one Compound I, wherein R1 and R5 each independently represent a hydrogen, a C1-C6 alkyl, a hydroxy, or a C1-C6 alkoxy; wherein R2, R3, and R4 each independently represent a hydrogen, a C1-C6 alkyl, or a C1-C6 alkoxy; wherein R6 and R7 each independently represent a hydrogen, a C1-C6 alkyl, a protecting group, or a directing group; wherein X represents a halo moiety or a halo-like moiety; wherein at least one of R1 and R5 represent a hydrogen; and provided that in Compound II, R7 represents a protecting group or a directing group, and either
(1) prior to step (ii), the at least one Compound III is combined with at least one deprotecting agent such that the protecting group or directing group represented by R7 is replaced with a hydrogen or a C1-C6 alkyl, or(2) prior to step (iii), the at least one Compound IV is combined with at least one deprotecting agent such that the protecting group or directing group represented by R7 is replaced with a hydrogen or a C1-C6 alkyl.