专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-10745354-B2 优先权日:2017-11-01 标题 :Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols 发明人:STOLTZ BRIAN M; NGAMNITHIPORN AURAPAT; JETTE CARINA I; BACHMAN SHOSHANA; VIRGIL SCOTT C; LACKNER SEBASTIAN 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic α-quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.
专利号:US-8729306-B2 优先权日:2010-02-05 标 题:Process for the preparation of nitrogen substituted aminotetralins derivatives 发明人:VASSELIN DAVID; CARLY NICOLAS; ATES CELAL 权利人:VASSELIN DAVID; CARLY NICOLAS; ATES CELAL; UCB PHARMA GMBH 摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines which synthesis comprises catalytic asymmetric hydrogenation of compounds of general formula (A).
专利号:US-2022064111-A1 优先权日:2019-01-17 标 题:Enantioselective synthesis of brivaracetam and intermediates thereof 发明人:ROY SARABINDU; GHOSH ANGSHUMAN; KUBEER RAMESH DHONDI; PRASAD MUTYALA V V VARA; PAUL GOPAL; GARAI ABHISHEK; CHAKRABORTY SOURAV; HALDAR ANIMESH; YADAW AJAY KUMAR; ROY SUBHO 权利人:CLININVENT RES PVT LTD 摘要:The present invention relates to an improved and economical process for enantioselective synthesis and purification of a novel key intermediate of Brivaracetam. Further, the present invention also relates to a process for the preparation of a chirally pure Brivaracetam of formula I utilizing the said intermediate.
专利号:US-2024199569-A1 优先权日:2022-11-30 标 题:Process for the manufacture of inhibitors of kras 发明人:ZHANG YONGDA; CHONG EUGENE; REEVES JONATHAN TIMOTHY; WHITE JADA A H; LEI ZHEN 权利人:BOEHRINGER INGELHEIM INT 摘要:This invention relates to an efficient and enantioselective synthesis of the spiro-compounds of formula (1) as common intermediate, featuring an asymmetric introduction of the all-carbon quaternary centre in high selectivity and a very efficient one-pot procedure for the C2 elongation to generate the spiro-structure.For the all-carbon quaternary centre, a Tsuji-Trost asymmetric allylic alkylation (AAA) process was designed to develop a sustainable procedure with very low catalyst loading, thereby also facilitating the Pd content control in the product, under practically solvent free conditions. Furthermore, multiple synthetic transformations in a one-pot procedure were implemented by using a one-pot procedure either in form of a three-transformation sequence comprising Hydroboration-Alkylation-Dieckmann Condensation to compound of formula (1) or in form of a five-transformation sequence comprising Hydroboration-Alkylation-Dieckmann Condensation-Hydrolysis-Decarboxylation to compound of formula (9).