专利号:US-10968174-B2 优先权日:2016-12-21 标题:Synthesis of a thiosulfonic acid by a step of periodate mediated oxidative coupling of a thiosulfonic acid with an aniline 发明人:SINCLAIR JAMES PETER; NICOLL SARAH LOUISE; STOREY JOHN MERVYN DAVID; LARCH CHRISTOPHER PAUL 权利人:WISTA LAB LTD 摘要:The present invention pertains generally to the field of chemical synthesis, and more particularly to methods for the chemical synthesis of a thiosulfonic acid of Formula (1) by a step of periodate mediated oxidative coupling of a thiosulfonic acid of Formula (2) with an aniline of Formula (3), as described herein. The present invention also relates to such methods which incorporate one or more additional (subsequent and/or preceding) steps, for example, to prepare compounds of Formula (5) from compounds of Formula (1); to prepare compounds of Formula (6) from compounds of Formula (5); and to prepare compounds of Formula (2) from compounds of Formula (4), as described herein.
专利号:US-11672829-B2 优先权日:2015-09-10 标 题:Genetically engineered coronavirus-specific effector cells for in situ synthesis of antiviral proteins 发明人:BHATNAGAR PARIJAT; SSEMADAALI MARVIN A 权利人:STANFORD RES INST INT 摘要:An example genetically engineered effector cell comprises an exogenous polynucleotide sequence that includes a receptor element, an actuator element, and an effector element. The receptor element encodes a chimeric antigen receptor (CAR) comprising an extracellular antigen binding domain operably linked to a transmembrane domain, and an intracellular signaling domain, wherein the extracellular antigen binding domain recognizes an antigen on a surface of a Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2)-infected cell. The actuator element encodes a transcription factor binding site that upregulates synthesis of an antiviral protein. The effector element encodes the antiviral protein operably linked to a signal peptide, wherein, in response to the antigen binding domain of the CAR binding to the antigen of SARS-CoV-2-infected cell, the engineered effector cell is configured to activate and, to synthesize and secrete the antiviral protein.
专利号:US-5703223-A 优先权日:1994-09-02 标题 :Solid phase synthesis of oligonucleotides with stereospecific substituted phosphonate linkages by pentavalent grignard coupling 发明人:WICKSTROM ERIC; LE BEC CHRISTINE 权利人:UNIV JEFFERSON 摘要:The present invention provides a method for producing an oligonucleotide having stereospecific substituted phosphonate linkages by use of a pentavalent Grignard coupling reaction on a solid phase support. The method can be used for automated synthesis of oligonucleotides having sequential equatorial or axial stereospecific substituted phosphonate linkages.
专利号:WO-2006046949-A1 优先权日:2004-10-22 标 题 :SYNTHESIS AND ANTIMALARIAL ACTIVITY OF PYRROLO[3,2-f]QUINAZOLINE-1,3- DIAMINE DERIVATIVES 发明人:AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R 权利人:WALTER REED ARMY INST OF RES W; AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R 摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P.vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs,. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.
专利号:US-8497375-B2 优先权日:2010-06-11 标 题 :Method of synthesis of ferroquine by convergent reductive amination 发明人:FEREY VINCENT; MATEOS-CARO JULIA; MONDIERE REGIS; VAYRON PHILIPPE; VIGNE SYLVIE 权利人:SANOFI SA 摘要:The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm): n n n n n n n n n n n n comprising a reaction of reductive amination, said reaction comprising: n (i) a stage of condensation of an aldehyde-amino ferrocene of formula (III), in which R represents a hydrogen atom or a methyl group, with 7-chloroquinolin-4-amine as shown below, n n n n n n n n n n n n n n n n followed by n (ii) a stage of reduction of the product of condensation obtained in the preceding stage and n (iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as