专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:US-5756745-A 优先权日:1994-05-31 标题 :Preparation of nalbuphine having low levels of β-epimer 发明人:KAVKA FRANK 权利人:MALLINCKRODT MEDICAL INC 摘要:A process is described for the synthesis of nalbuphine. The process results in a product having very low levels of the undesirable β-epimer. The process is a five-step synthesis that begins with a compound such as an N,O 3 -bis (alkoxycarbonyl) -14-hydroxynormorphinone.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-11091445-B2 优先权日:2016-10-24 标题 :Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders 发明人:RUCH WERNECK GUIMARÃES CRISTIANO; FELYPE ZANETI DE AZEVEDO HATYLAS; MASCARELLO ALESSANDRA; WATANABE DA COSTA RENATA; FREIRE TORRES RUSSO VALTER; MANNOCHIO DE SOUZA RUSSO ELISA 权利人:ACHE LABORATORIOS FARMACEUTICOS SA 摘要:The present disclosure relates to novel and inventive pharmacologically active benzimidazole derivative compounds, which surprisingly have high affinity for melatonin MT1 and MT2 receptors and low affinity for CYP450 complex enzymes, specially CYP1A2. The present invention also relates to novel and inventive routes of synthesis of these compounds, pharmaceutical compositions comprising the compounds and the use of these compounds in the treatment of individuals affected by psychiatric disorders and/or sleep disorders related to these receptors (specially depression, anxiety, circadian cycle disorders), in addition to a process for producing the composition.
专利号:US-4202982-A 优先权日:1976-03-23 标 题 :Process for the preparation of 14-hydroxymorphinan derivatives 发明人:BACHAND CAROL; MONKOVIC IVO; WONG HENRY 权利人:BRISTOL MYERS CO 摘要:N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorphinan has been found to possess potent agonist/antagonist activity as a non-narcotic analgesic. A new and efficient total synthesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline.
专利号:US-4089855-A 优先权日:1976-04-23 标题:Process for the stereoselective reduction of 6- and 8-keto morphine and morphinan derivatives with formamidinesulfinic acid and compounds obtained thereby 发明人:CHATTERJIE NITHIANANDA; INTURRISI CHARLES E 权利人:CORNELL RES FOUNDATION INC 摘要:Process for the stereoselective synthesis of 6β-and 8β- hydroxy epimers by the chemical reduction of 6- and 8-keto derivatives in the morphine and morphinan series utilizing alkaline formamidinesulficic acid. The 6β- and 8β-hydroxy derivatives obtained according to the invention evidence narcotic antagonist and/or agonist activity and are also useful in the chemical and pharmacological standardization of various morphine and codeine derivatives and metabolites.