Novel chemoselective reduction of the tetrahydro-4-pyridyl versus indole moiety governed by electron donation: first X-ray evidence for indolopiperidyl–borane complexation
摘要:
A series of amino-borane complexes of structure type 2 are the key intermediates in the preparation of 3-(piperidyl) indole derivatives. The selective reduction of the tetrahydro-4-pyridyl double bond via 2 under strongly acidic conditions is feasible only when the pyridyl double bond is conjugated with electron rich substituents, such as indoles. This reduction methodology allows the presence of reducible and hydrogenolizable functional groups. An improved process to prepare 2 by treatment of the 3-(tetrahydro-4-pyridyl) indole derivatives with NaBH4 in THF under acidic conditions (AcOH or CF3COOH) is also described. (C) 2002 Elsevier Science Ltd. All rights reserved.
ARYLPIPERAZINE-CONTAINING PURINE DERIVATIVES AND USES THEREOF
申请人:Lee Jinhwa
公开号:US20120232090A1
公开(公告)日:2012-09-13
A novel arylpiperazine-containing purine derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating depressive disorders, are provided.
一种含有芳基哌嗪的嘌呤衍生物以及包含其作为活性成分的药物组合物被提供,用于预防或治疗抑郁症。
PHARMACEUTICAL COMPOUNDS
申请人:——
公开号:US20010053783A1
公开(公告)日:2001-12-20
A pharmaceutical compound of the formula
1
in which R
1
is hydrogen, C
1-4
alkyl, C
1-4
alkoxy or halo, and R
2
is hydrogen, C
1-4
alkyl or C
1-4
alkoxy; or a salt thereof.
NOVEL ARYLPIPERAZINE-CONTAINING IMIDAZOLE 4-CARBOXAMIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
申请人:Lee Jinhwa
公开号:US20120115881A1
公开(公告)日:2012-05-10
A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.
Substituted 4-(6-fluoro-[1H]-indol-3-yl)-1,2,3,6-tetrahydropyridine for the treatment of CNS-disorders
申请人:ELI LILLY AND COMPANY LIMITED
公开号:EP0854146A1
公开(公告)日:1998-07-22
A pharmaceutical compound of the formula
in which R1 is hydrogen, C1-4 alkyl, C1-4 alkoxy or halo, and R2 is hydrogen, C1-4 alkyl or C1-4 alkoxy; or a salt thereof.
The compounds of the invention and their pharmaceutically acceptable salts are indicated for use in the treatment of disorders of the central nervous system.