专利号:WO-2018108954-A1 优先权日:2016-12-12 标题 :Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 发明人:GOSSELIN FRANCIS; LINGHU XIN 权利人:HOFFMANN LA ROCHE; GENENTECH INC 摘要:Methods of making 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 9, an intermediate useful for the synthesis of estrogen receptor modulating compounds are described.
专利号:US-6255315-B1 优先权日:1997-06-18 标题:Alpha 1a adrenergic receptor antagonists 发明人:PATANE MICHAEL A; SELNICK HAROLD G; BOCK MARK G 权利人:MERCK & CO INC 摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha relductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
专利号:CN-113214255-B 优先权日:2021-04-22 标题:Synthesis method of 2,6-diazaspiro[3.5]nonane-6-carboxylic acid tert-butyl ester and its salts
参考文献:10.1055/s-0030-1261181 摘要:Augustine J, Bombrun A, Atta R. A Practical and Cost-Efficient, One-Pot Conversion of Aldehydes into Nitriles Mediated by ‘Activated DMSO’. Synlett. 2011 Aug 12;2011(15):2223–7. doi: 10.1055/s-0030-1261181.