专利号:US-2007129554-A1 优先权日:2005-10-24 标题 :Alpha functionalization of cyclic, ketalized ketones and products therefrom 发明人:HARRINGTON PETER J; KHATRI HIRALAL N; KHATRI SUDHA 权利人:HARRINGTON PETER J; KHATRI HIRALAL N; KHATRI SUDHA 摘要:Methodologies for the alpha-monohalogenation of acid sensitive ketones, especially cyclic, acid-sensitive, ketalized ketones. As one approach, the ketone is reacted with a halogen donor compound, e.g., N-chlorosuccinimide, in anhydrous, highly polar organic reagents such as dimethylformamide (DMF). As another monohalogenation approach, it has been observed that organic salts generated from amines and carboxylic acids catalyze the monohalogenation of ketalized ketone in reagents comprising alcohol solvent (methanol, ethanol, isopropanol, etc.). The monohalogenation is fast even at −5° C. The salt can be rapidly formed in situ from ingredients including amines and/or carboxylic acids without undue degradation of the acid sensitive ketal. Aryl ketones are monooxygenated using iodosylbenzene. This methodology is applied to monohalogenation of an acid sensitive monoketal ketone. The ability to prepare monohalogenated, acid sensitive ketones facilitates syntheses using halogenated, acid sensitive ketones. As just one example, facile synthesis of halogenated, acid sensitive ketones provides a new approach to synthesize the S-ketal-acid S-MBA (S-methylbenzylamine) salt useful as an intermediate in the manufacture of a glucokinase activator. As an overview of this scheme, a monohalogenated, cyclic, ketalized ketone is prepared using monohalogenation methodologies of the present invention. The halogenated compound is then subjected to a Favorskii rearrangement under conditions to provide the racemic acid counterpart of the desired chiral salt. The desired chiral salt is readily recovered in enantiomerically pure form from the racemic mixture.
专利号:EP-0388789-A1 优先权日:1989-03-18 标 题 :Process for the production of enantiomers of hetrazepines 发明人:STRANSKY WERNER DR; LANGBEIN ADOLF DR; BRANDT KLAUS DR; WEBER KARL-HEINZ DR; WALTHER GERHARD DR 权利人:BOEHRINGER INGELHEIM KG; BOEHRINGER INGELHEIM INT 摘要:The invention relates to an improved process for the preparation of enantiomerically pure hetrazepines by a stereospecific synthesis starting from cyclopentane-3-carboxylic acid esters.
专利号:SU-736579-A1 优先权日:1978-12-08 标题:Ethyl esters of 2-(omega-bromoalkyl) cyclopentanone-3-carboxylic acid as starting products for synthesis of biologically active prostaglandins or their analogs and method for preparing the same
专利号:US-9861636-B2 优先权日:2014-04-29 标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors 发明人:HE WEI 权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD 摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
专利号:CN-117964497-A 优先权日:2024-01-26 标题:A kind of synthesis method of 3,3-difluorocyclopentylamine hydrochloride
[参考文献]: Dieter F Münzer, Et Al. Stereoselective Hydroxylation Of An Achiral Cyclopentanecarboxylic Acid Derivative Using Engineered P450S Bm-3. Chem Commun (Camb). 2005 May 28:(20):2597-9.
合成参考文献
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