Neo-Hexylboronic Acid置于chromium(Vi) Oxide体系中,用 二氯甲烷,溶剂黄146 用作溶剂,化学反应 12.0H,以80%的收率获得3,3-二甲基-1-丁酸 参考文献:A Convenient Procedure For The Direct Conversion Of Terminal Alkenes Into Carboxylic Acids 标题:A Convenient Procedure For The Direct Conversion Of Terminal Alkenes Into Carboxylic Acids 摘要:Alkylboronic Acids,Readily Synthesized From A Variety Of Representative Terminal Alkenes Via Hydroboration With Dibromoborane-Methyl Sulfide,Undergo A Facile Oxidation With Chromium Trioxide In 90% Aqueous Acetic Acid To Provide Carboxylic Acids In 80-97% Isolated Yields,Without Rearrangement Or Loss Of Carbon. Doi:10.1016/s0040-4039(00)91853-7
专利号:US-11667658-B2 优先权日:2021-06-30 标 题:Chemical synthesis of the organoarsenical antibiotic arsinothricin 发明人:ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN 权利人:ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
专利号:US-2022298204-A1 优先权日:2019-07-05 标题 :Synthesis of a-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:US-11639349-B2 优先权日:2020-05-28 标题:Stereoselective synthesis of intermediate for preparation of heterocyclic compound 发明人:CHEN WEN-CHANG; HSU HAN-PEI; CHOU SHAN-YEN; CHUANG SHIH-CHIEH; YEN CHI-FENG 权利人:TAI GEN BIOTECHNOLOGY CO LTD; TAIGEN BIOPHARMACEUTICALS CO BEIJING LTD; TAIGEN BIOTECHNOLOGY CO LTD 摘要:Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.
专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-9957355-B2 优先权日:2013-06-12 标 题 :Device and method for synthesis of a polymer under separation of a gaseous substance 发明人:ZHU NING; STAMMER ACHIM; CLAUSS JOACHIM; KORY GAD 权利人:BASF SE 摘要:The invention relates to a device for synthesis of a polymer under separation of a gaseous substance. Said device comprises a reaction chamber ( 1 ), which has a top section ( 11 ), a middle section ( 12 ) and a bottom section ( 13 ), an inlet opening ( 2 ) which is arranged in the middle section ( 12 ), a first outlet opening ( 3 ) which is arranged in the bottom section ( 13 ), a second outlet opening ( 4 ) which is arranged in the top section ( 11 ), a first return opening ( 51 ), which is arranged in the bottom section ( 13 ), a second outlet opening ( 52 ), which is arranged under the top section ( 11 ), a distribution device ( 6 ), which is arranged between the top section ( 11 ) and the middle section ( 12 ), and a removal device ( 7 ) which is arranged to be movable along the top section ( 11 ). The invention further relates to a method for synthesis of a polymer which can be carried out in said device.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
摘要:Chemler, S. R.; Kennedy-Ellis, J. J., Science of Synthesis: Special Topics, (2022) 1, 105. 摘要:Cellnik, T.; Jo, W.; Healy, A., Science of Synthesis: Knowledge Updates, (2024) 2, 371. 摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 210. 摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 214. 摘要:de Figueiredo, R. M., Science of Synthesis: Knowledge Updates, (2024) 2, 306.