PROCESS-DEVELOPMENT OF OXY-4-PYRIMIDINYL)-1-PIPERAZINYL]PROPYL]-1H-INDOLE DIHYDROCHLORIDE

Authors
ANDERSON NG ARY TD BERG JL BERNOT PJ CHAN YY CHEN CK DAVIES ML DIMARCO JD DENNIS RD DESHPANDE RP DO HD DROGHINI R EARLY WA GOUGOUTAS JZ GROSSO JA HARRIS JC HAAS OW JASS PA KIM DH KODERSHA GA KOTNIS AS LAJEUNESSE J LUST DA MADDING GD MODI SP MONIOT JL NGUYEN A PALANISWAMY V PHILLIPSON DW SIMPSON JH THORAVAL D THURSTON DA TSE K POLOMSKI RE WEDDING DL WINTER WJ
Citation
Ng. Anderson et al., PROCESS-DEVELOPMENT OF OXY-4-PYRIMIDINYL)-1-PIPERAZINYL]PROPYL]-1H-INDOLE DIHYDROCHLORIDE, Organic process research & development, 1(4), 1997, pp. 300-310
Citations number
47
Journal title
Organic process research & development → ACNP
ISSN journal
10836160
Volume
1
Issue
4
Year of publication
1997
Pages
300 - 310
Database
ISI
SICI code
1083-6160(1997)1:4<300:POO>2.0.ZU;2-A
Abstract
xy-4-pyrimidinyl)-1-piperazinyl]-propyl]-1H-indole dihydrochloride (1) facilitates 5-HT neurotransmission and was an antidepressant drug can didate. The development of a safe, rugged process for the large-scale, chromatography-free preparation of this compound is described, The ma in areas of optimization included a Fischer indole synthesis, preparat ion and chlorination of a monohydroxypyrimidine, and coupling of the r esultant fragments to prepare the drug substance.