Process for preparing histone deacetylase inhibitors and...

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acids and salts thereof

Reexamination Certificate

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C556S413000, C556S423000, C562S459000

Reexamination Certificate

active

11108858

ABSTRACT:
A process for preparing unsaturated esters useful as intermediates for HDAC inhibitors, by reacting an aldehyde or ketone having the following formula I:wherein R1is an aromatic group or a combined aliphatic and aromatic group; X is —O—, —S—, —COO—, —OOC—, —CONR7—, or —R7NCO—; L1an aliphatic linking group, an aromatic linking group, or a combined aliphatic and aromatic linking group; R2and R3are each independently hydrogen, a hydroxy group, an alkoxy group, an amino group, a carboxyl group, an amide group, an ester group, a carbamate group, an aliphatic group, an aromatic group, a combined aliphatic and aromatic group, R2and R3together are ═O, or one of R2and R3form a double bond with one of R4and R5; R4and R5are each independently hydrogen, a hydroxy group, an alkoxy group, an amino group, a carboxy group, an amide group, an ester group, a carbamate group, an aliphatic group, an aromatic group, a combined aliphatic and aromatic group, or one of R4and R5form a double bond with one of R2and R3; R6is hydrogen, an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; R7is hydrogen, an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; m is 0 or 1; n is 0 or 1; and p is 0 or 1; with an ester having the following formula II:wherein R8is an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; R9and R10each independently hydrogen, an aliphatic group, an aromatic group, a combined aliphatic and aromatic group, or one of R9and R10form a double bond with L2; R11and R12are each an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; L2is an aliphatic linking group, an aromatic linking group, or a combined aliphatic and aromatic linking group; A is P or As; and p is 0 or 1.

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