2006Qilu Pharmaceutical AffairsRequires access

Synthesis of 4-Amino-5-chloro-2-ethoxy-N-4-(4-fluorobenzyl)-2-morpholinylmethyBenzamide

Ziying Jiang

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Abstract

OBJECTIVE To synthesize 4-amino-5-chloro-2-ethoxy-N-4-(4- fluorobenzyl)-2- morpholinylmethy benzamide .METHODS The target compound was synthesized from 4-amino-5-chloro-2-ethoxy benzoic acid and intermediate B and C.RESULTS The yield of the target compound was improved to 90.0%,up to ahout 30.0%.All of the intermediates were made in Lu′nan Pharmaceutical Better Limited Corporation and verified by us.CONCLUSION The recycle rate was improved and the cost was decreased by changing the path of synthesis.And the technique is suitable for industrial production.

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OBJECTIVE To synthesize 4-amino-5-chloro-2-ethoxy-N-4-(4- fluorobenzyl)-2- morpholinylmethy benzamide .METHODS The target compound was synthesized from 4-amino-5-chloro-2-ethoxy benzoic acid and intermediate B and C.RESULTS The yield of the target compound was improved to 90.0%,up to ahout 30.0%.All of the intermediates were made in Lu′nan Pharmaceutical Better Limited Corporation and verified by us.CONCLUSION The recycle rate was improved and the cost was decreased by changing the path of synthesis.And the technique is suitable for industrial production.

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Available abstract

OBJECTIVE To synthesize 4-amino-5-chloro-2-ethoxy-N-4-(4- fluorobenzyl)-2- morpholinylmethy benzamide .METHODS The target compound was synthesized from 4-amino-5-chloro-2-ethoxy benzoic acid and intermediate B and C.RESULTS The yield of the target compound was improved to 90.0%,up to ahout 30.0%.All of the intermediates were made in Lu′nan Pharmaceutical Better Limited Corporation and verified by us.CONCLUSION The recycle rate was improved and the cost was decreased by changing the path of synthesis.And the technique is suitable for industrial production.

Key concepts: Benzamide, Alkoxy group, Yield (engineering), Benzoic acid, Chemistry, Amino acid, Combinatorial chemistry, Medicinal chemistry

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