专利号:US-9790206-B2 优先权日:2013-02-27 标 题:Intermediates for use in the preparation of indazole derivatives and processes for the preparation thereof 发明人:EARY C TODD; HACHE BRUNO P; JUENGST DERRICK; SPENCER STACEY RENEE; STENGEL PETER J; WATSON DANIEL JOHN 权利人:ARRAY BIOPHARMA INC 摘要:Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processes described herein.
专利号:US-4536599-A 优先权日:1978-08-22 标题:Synthesis of amine derivatives 发明人:MASUKO FUJIO; KATSURA TADASHI 权利人:SUMITOMO CHEMICAL CO 摘要:An amine of the formula, ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are each hydrogen, alkyl or the like and n is 1, 2 or 3, including α-phenyl-β-(p-tolyl)-ethylamine, which is useful as an optically resolving agent, an intermediate of medicines and the like, is effectively produced by a novel process comprising hydrolysis of the corresponding nitrile of the formula, ##STR2## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above, followed by alkali-decomposition of the resulting amide of the formula, ##STR3## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above. An amide including the above one is effectively produced by hydrolysis of the corresponding nitrile in the presence of a base and hydrogen peroxide using an organic quaternary ammonium salt and/or a tertiary amine as a catalyst.
专利号:US-6235759-B1 优先权日:1998-10-29 标 题 :Dihydropyridinones and pyrrolinones useful as alpha 1A adrenoceptor antagonists 发明人:BARROW JAMES C; NANTERMENT PHILIPPE G; SELNICK HAROLD G 权利人:MERCK & CO INC 摘要:Novel dihydropyridinone and pyrrolinone compounds and pharmaceutically acceptable salts thereof 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 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:EP-0008532-A1 优先权日:1978-08-22 标 题 :Synthesis of amines
专利号:EP-0008532-B1 优先权日:1978-08-22 标 题 :Synthesis of amines
专利号:EP-0040896-A2 优先权日:1978-08-22 标 题 :Synthesis of amides