Bristol-myers Squibb Compnay

Andrew D Williams

Edward H Ruediger

Joseph P Yevich

David W Smith

Ronald J Mattson

Bradley C Pearce

Michael J Humora

Keith D Combrink

Frank D Yocca

Sandeep P Modi

Sushi K Srivastava

An improved, novel convergent process suitable for large scale preparation of the antimigraine agent 4-(5-methoxy-4-pyrimidinyl)-1-[3-[5-[[(methylamino)sulfonyl]methyl]-1H-ind ol-3-yl]propyl]piperazine (BMS 180048) and close analogs. The improved process provides efficiencies in handling, purification, and product yield and involves a novel heteroannulation reaction that provides the indole ring moiety and propylpiperazinyl-pyrimidine backbone in a single step.

Process for large-scale production of indolyl alkyl pyrimidinyl

A series of novel alkoxypyridin-4-yl and alkoxypyrimidin-4-yl derivatives of indol-3-ylalkylpiperazines of Formula I are intended to be useful agents ##STR1## for alleviation of vascular headache on the basis of their potent affinity and agonist activity at 5-HT1D binding sites.

Antimigraine 4-pyrimidinyl and pyridinyl derivatives of

A series of novel indol-3-ylalkyl derivatives of alkoxypyrimidinylpiperazines are disclosed as Formula I. ##STR1## These compounds are intended to be useful agents for alleviation of vascular headache on the basis of their potent affinity and agonist activity at 5-HT1D binding sites.

Indolylalkyl derivatives of pyrimidinylpiperazine for treating vascular

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Middletown, CT, United States of America

Andrew D Williams