preferable for expression of potent analgesicactivity, and that the free carboxyl group is superior in its analgesicactivity to that of the esterified or amidated carboxy group at the C-terminal. In addition, N-methylation of the amide bond at the 4th position contributed to improved analgesicactivity. These results indicated that the strong and long-lasting analgesic effect of ADAMB is expressed by
Disclosed are compounds Formula I
1
and pharmaceutically acceptable salts thereof, wherein R
1
, R
2
, R
4
, and R
5
are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Disclosed are compounds Formula I
and pharmaceutically acceptable salts thereof, wherein R
1
, R
2
, R
4
, and R
5
are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
3a-(o-Nitrophenyl)octahydroindol-4-ones: Synthesis and spectroscopic analysis
作者:Daniel Solé、Joan Bosch、Josep Bonjoch
DOI:10.1016/s0040-4020(96)00065-8
日期:1996.3
A short entry to 3a-(o-nitrophenyl)octahydroindol-4-ones employing ozonolysis and double reductive amination of 2-allyl-2-(o-nitrophenyl)-1,3-cyclohexanedione (9) is described. The symmetric dione 9 is synthesized in a 50% overall yield from 1,3-cyclohexanedione by means of o-nitroarylation followed by O-allylation and subsequent Claisen rearrangement. Configurational and conformational aspects of azabicyclic derivatives 1 (a-k) are discussed.
PROCESS FOR THE PREPARATION OF (S)-2-AMINO-1-PROPANOL (L-ALANINOL) FROM (S)-1-METHOXY-2-PROPYLAMINE
申请人:Kutzki Olaf
公开号:US20100240928A1
公开(公告)日:2010-09-23
The invention relates to a process for the preparation of (S)-2-amino-1-propanol (L-alaminol) from (S)-1-methoxy-2-propylamine via the hydrochloride of (S)-2-amino-1-propanol and subsequent work-up.