专利号:US-8461384-B2 优先权日:2006-12-11 标 题 :Preparation of amides from an acid and amine for intermediates in the synthesis of morphinans 发明人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L 权利人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L; MALLINCKRODT LLC 摘要:The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl 3 that is necessary to form the 3,4-dihydroisoquinoline.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:US-2009247761-A1 优先权日:2006-12-11 标 题:Preparation of 3,4-Dihydroisoquinolines in the Synthesis of Morphinans
专利号:US-2012016390-A1 优先权日:2010-07-16 标 题 :Bioadhesive compounds and methods of synthesis and use 发明人:LEE BRUCE P; MURPHY JOHN L; VOLLENWEIDER LAURA; DALSIN JEFFREY L; LYMAN ARINNE N 权利人:LEE BRUCE P; MURPHY JOHN L; VOLLENWEIDER LAURA; DALSIN JEFFREY L; LYMAN ARINNE N; KNC NER ACQUISITION SUB INC 摘要:The invention describes new synthetic medical adhesives and antifouling coatings which exploit the key components of natural marine mussel adhesive proteins.
专利号:US-8232400-B2 优先权日:2006-12-11 标 题 :Preparation of 3,4-dihydroisoquinolines in the synthesis of morphinans
专利号:EP-2161253-A2 优先权日:2006-12-11 标 题 :Process for the preparation of 3,4-dihydroisoquinolines in the synthesis of morphinans
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合成参考文献
参考文献:10.1212/wnl.47.4.1037 摘要:Pappert EJ, Tangney CC, Goetz CG, Ling ZD, Lipton JW, Stebbins GT, Carvey PM. Alpha-tocopherol in the ventricular cerebrospinal fluid of Parkinson's disease patients: dose-response study and correlations with plasma levels. Neurology. 1996 Oct;47(4):1037–42. doi: 10.1212/wnl.47.4.1037.