专利号:US-2007293706-A1 优先权日:2004-11-01 标 题:Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones 发明人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 权利人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 摘要:1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.
专利号:US-2008171873-A1 优先权日:2007-01-12 标题:Synthesis of selected stereoisomers of certain substituted alcohols 发明人:HARMS ARTHUR E 权利人:HARMS ARTHUR E 摘要:A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric amine with a halogen-substituted heterocyclic compound, or a stereoisomeric ketone or aldehyde with an amino-substituted heterocyclic compound. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.
专利号:US-2011137038-A1 优先权日:2006-11-09 标题 :Synthesis of selected stereoisomers of certain substituted alcohols 发明人:HARMS ARTHUR E 权利人:HARMS ARTHUR E 摘要:A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric epoxide with an amine, a carboxylic acid, an amide, a sulfonyl, or a cyanide. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.
专利号:US-2008114172-A1 优先权日:2006-11-09 标 题 :Synthesis of Selected Stereoisomers of Certain Substituted Alcohols
专利号:US-6316437-B1 优先权日:1999-09-30 标题:Spirohydantoin compounds and uses thereof 发明人:HOFFMAN JACOB M 权利人:MERCK & CO INC 摘要:Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically 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 reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-2023002426-A1 优先权日:2019-11-15 标题 :Chiral synthesis of a tertiary alcohol