专利号:US-9518034-B2 优先权日:2013-10-14 标题 :Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof 发明人:STOLTZ BRIAN M; DOUGHERTY DENNIS A; DUQUETTE DOUGLAS; DUFFY NOAH 权利人:CALIFORNIA INST OF TECHN 摘要:This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n ncomprising treating a compound of formula (II):n n nwith a transition metal catalyst under alkylation conditions.
专利号:US-11377396-B2 优先权日:2014-12-18 标题 :Enantioselective synthesis of α-quaternary Mannich adducts by palladium-catalyzed allylic alkylation 发明人:STOLTZ BRIAN M; NUMAJIRI YOSHITAKA; PRITCHETT BEAU P; CHIYODA KOJI 权利人:CALIFORNIA INST OF TECHN 摘要:This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n ncomprising treating a compound of formula (II):n n nwith a transition metal catalyst under alkylation conditions.
专利号:US-2016096810-A1 优先权日:2014-10-07 标 题 :Enantioselective synthesis of dialkylated n,o-heterocycles by palladium-catalyzed allylic alkylation 发明人:STOLTZ BRIAN M; NUMAJIRI YOSHITAKA; BEHENNA DOUGLAS C 权利人:STOLTZ BRIAN M; NUMAJIRI YOSHITAKA; BEHENNA DOUGLAS C 摘要:This invention provides enantioenriched N,O-heterocyclic compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n n n n n n n n n n comprising treating a compound of formula (II): n n n n n n n n n n with a transition metal catalyst under alkylation conditions.
专利号:US-9403766-B2 优先权日:2008-01-17 标 题:Intermediates for producing NEP inhibitors or prodrugs thereof 发明人:HOOK DAVID; RISS BERNARD; KAUFMANN DANIEL; NAPP MATTHIAS; BAPPERT ERHARD; POLLEUX PHILIPPE; MEDLOCK JONATHAN; ZANOTTI-GEROSA ANTONIO 权利人:HOOK DAVID; RISS BERNARD; KAUFMANN DANIEL; NAPP MATTHIAS; BAPPERT ERHARD; POLLEUX PHILIPPE; MEDLOCK JONATHAN; ZANOTTI-GEROSA ANTONIO; NOVARTIS AG 摘要:The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, n nwherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
专利号:US-2020157020-A1 优先权日:2014-12-18 标题:Enantioselective synthesis of alpha-quaternary mannich adducts by palladium-catalyzed allylic alkylation
专利号:US-2015105552-A1 优先权日:2013-10-14 标 题 :Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof