141071-86-5Relevant articles and documents
3-CYANOANILINOALKYLARYLPIPERAZINE DERIVATIVE AND USE THEREOF IN PREPARING DRUGS
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Paragraph 0088; 0089, (2015/04/21)
Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and go
An efficient Fischer indole synthesis of avitriptan, a potent 5-HT(1D) receptor agonist
Brodfuehrer,Chen,Sattelberg T.R.,Smith,Reddy,Stark,Quinlan,Reid
, p. 9192 - 9202 (2007/10/03)
An efficient synthesis of antimigraine drug candidate avitriptan (1, BMS 180048) is reported. The key step is a two-phase Fischer indolization reaction between hydrazine 6 and 5-chlorovaler-aldehyde, 20, to give the chloropropylindole 35, which is susceptible to acid-catalyzed degradation under the reaction conditions required for its formation. Sequential coupling of 35 with piperazine, 26, and 4-chloro-5-methoxypyrimidine, 24, gives the title compound in 40-45% overall yield. Significant improvements in the syntheses of the known starting materials, hydrazine 6, 5- chlorovaleraldehyde, 20, and 4-chloro-5-methoxypyrimidine, 24, were also achieved.
INDOLYLALKYL DERIVATIVES OF PYRIMIDINYLPIPERAZINE FOR TREATING VASCULAR HEADACHE
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, (2008/06/13)
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.