[(2R,3R,5R)-3-Benzoyloxy-5-(2,4-Dioxo-1,3-Diazinan-1-yl)-4,4-Difluorooxolan-2-Yl]Methyl Benzoate置于cerium(III) Chloride Heptahydrate,氨,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 甲醇,乙醇,二氯甲烷,水,乙腈 用作溶剂,化学反应 119.08H,反应生成西达尿苷 参考文献: Synthetic Route To 2'-Deoxy-2',2'-Difluorotetrahydrouridines[fr] Voie De Synthèse Pour 2'-Désoxy-2',2'-Difluorotétrahydrouridines 标题: Synthetic Route To 2'-Deoxy-2',2'-Difluorotetrahydrouridines[fr] Voie De Synthèse Pour 2'-Désoxy-2',2'-Difluorotétrahydrouridines 摘要:本发明涉及合成2'-脱氧-2',2'-二氟四氢尿苷化合物的方法和中间体.
专利号:US-10954178-B1 优先权日:2020-08-28 标题 :Synthesis of haloindenes 发明人:WNUK STANISLAW F; HOWLADER MD ABU HASAN 权利人:WNUK STANISLAW F; HOWLADER MD ABU HASAN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides an expedited synthesis of 5, 6, and 7-iodoindenes from the corresponding aminoindan-1-ones in more than 70% yield, employing readily available precursors and reagents. A three-step sequence involves diazotization-iodination of aminoindan-1-one followed by reduction and dehydration. The method has a general character and can be extended for the preparation of various 4-, 5-, 6- or 7-haloindenes using different halogen sources for diazotization-halogenation reaction.
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-10889599-B2 优先权日:2018-02-27 标 题:1,1-diborylalkyl-1-metal compounds, preparation method thereof, and their applications toward synthesis of 1,1-diboronate ester compounds 发明人:CHO SEUNG HWAN; LEE YEOSAN 权利人:POSTECH ACAD IND FOUND 摘要:The present invention relates to a 1,1-diborylalkyl-1-metal compound including one metal group together with two identical boron groups at the sp3 carbon center, and its use. Specifically, the present invention relates to development of novel organic reactions, synthesis of functional molecules, and synthesis of new drugs by applying the novel 1,1-diboryl-1-metal substituted alkyl compounds to various molecular libraries which could not be synthesized by conventional methodologies.
专利号:US-9809566-B2 优先权日:2012-09-06 标题:Organocatalytic process for asymmetric synthesis of decanolides 发明人:RAWAT VARUN; DEY SOUMEN; SHELKE ANIL MARUTI; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.
专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
专利号:US-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.