Solvent and in situ catalyst preparation impacts upon Noyori reductions of aryl-chloromethyl ketones: application to syntheses of chiral 2-amino-1-aryl-ethanols
摘要:
As part of medicinal chemistry efforts we found it necessary to develop general syntheses of highly enantiomerically enriched 1-aryl-2-chloroethanols and 1-aryl-2-methylaminoethanols. A survey of literature methods suggested that a truly general approach had not yet been reported, encouraging us to undertake the development of such a methodology. This study describes the design, development, and reduction to practice of a general synthesis of chiral 1-aryl-2-chloroethanols and the transformation of these entities to highly enantiomerically enriched 1-aryl-2-methylaminoethanols. Of particular importance were observations of the impact of solvent and the method of catalyst preparation on the yield and enantiomerical excess of chlorohydrins prepared via Noyori transfer hydrogenations of aryl-chloromethyl ketones. (c) 2006 Elsevier Ltd. All rights reserved.
2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
申请人:——
公开号:US20030078260A1
公开(公告)日:2003-04-24
This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
这项发明涉及新颖的2,6-取代的色苷衍生物,可用于治疗β-3肾上腺素受体介导的疾病。
PROCESS FOR PREPARATION OF (S)-ALPHA-HALOME THYLPYRIDINE METHANOL DERIVATIVES
申请人:KANEKA CORPORATION
公开号:EP1454899A1
公开(公告)日:2004-09-08
The present invention provides a process for easily preparing a (S)-α-halomethylpyridine-methanol derivative, which is useful as an intermediate of pharmaceutical products, from inexpensive raw materials. The (S)-α-halomethylpyridine-methanol derivative is prepared by (S)-selectively reducing a 2-haloacetylpyridine derivative using an enzyme source having ability to (S)-selectively reduce a carbonyl group of the 2-haloacetylpyridine derivative, which can be obtained inexpensively. Also, a hydrohalic acid salt of (S)-α-halomethyl-3-pyridine-methanol derivative is isolated and purified as crystal from a (S)-α-halomethyl-3-pyridine-methanol derivative containing impurities using hydrohalic acid and an organic solvent.
[EN] COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND OBESITY<br/>[FR] TRAITEMENT COMBINE DU DIABETE ET DE L'OBESITE
申请人:MERCK & CO., INC.
公开号:WO1997016189A1
公开(公告)日:1997-05-09
(EN) The combination of the $g(b)3 adrenergic receptor agonist Compound A and a compound which modifies feeding behavior (e.g., the OB protein) is useful in the treatment of obesity and diabetes, either as compounds, pharmaceutically acceptable salts, pharmaceutical compoisition ingredients. Methods of treating obesity and diabetes are also described.(FR) L'invention porte sur la combinaison d'un composé A agoniste du récepteur adrénergique $g(b)3 et d'un composé modifiant le comportement alimentaire (par exemple la protéine OB) qui s'avèrent utiles contre l'obésité et le diabète. En utilisant soit la composition elle-même, soit ses sels pharmacocompatibles, soit des préparations pharmaceutiques dont ils sont les principes actifs. L'invention porte également sur les procédés de traitement associés.
Process for preparation of (s)-alpha-halomethylpyridine-methanol derivatives
申请人:——
公开号:US20040265991A1
公开(公告)日:2004-12-30
The present invention provides a process for easily preparing a (S)-&agr;-halomethylpyridine-methanol derivative, which is useful as an intermediate of pharmaceutical products, from inexpensive raw materials. The (S)-&agr;-halomethylpyridine-methanol derivative is prepared by (S)-selectively reducing a 2-haloacetylpyridine derivative using an enzyme source having ability to (S)-selectively reduce a carbonyl group of the 2-haloacetylpyridine derivative, which can be obtained inexpensively. Also, a hydrohalic acid salt of (S)-&agr;-halomethyl-3-pyridine-methanol derivative is isolated and purified as crystal from a (S)-&agr;-halomethyl-3-pyridine-methanol derivative containing impurities using hydrohalic acid and an organic solvent.