3-Cyanobenzaldehyde Oxime置于硫酰氟,Sodium Carbonate体系中,用 二甲基亚砜 作为反应溶剂,化学反应 12.0H,以251 Mg的收率获得产物间苯二甲腈 参考文献:使用dmso中的无机试剂nH2Oh / Na 2 Co 3 / So 2 F 2将醛(rcho)直接转化为腈(rcn)的级联过程 标题:使用dmso中的无机试剂nH2Oh / Na 2 Co 3 / So 2 F 2将醛(rcho)直接转化为腈(rcn)的级联过程 摘要:使用无机试剂(nH2Oh / Na 2 Co)开发了一种简单,温和且实用的方法,将醛直接转化为腈,可在较宽的底物范围内实现出色的官能团耐受性(52个实例,大多数情况下产率超过90%)3 / So 2 F 2)在dmso中.该方法允许以易用,原子和步经济的方式将易于获得,廉价且丰富的醛转化为高度有价值的腈,而无需过渡金属.该协议将作为将氰基部分安装到复杂分子的强大工具. DOI:10.1021/acs.Joc.8B03164
专利号:US-2023295162-A1 优先权日:2020-08-06 标 题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity 发明人:CSÃ?MPAI ANTAL; BÃ?RÃ?NY PÉTER; CZUCZI TAMÃ?S; Kovács Imre; ADAMIS BÃ?LINT; NÉMETH ZSÓFIA; MURÃ?NYI JÓZSEF; OLÃ?HNÉ SZABÓ RITA; BOSZE SZILVIA; MEZO GÃ?BOR; KOHIDAI LÃ?SZLÓ; LAJKÓ ESZTER; TAKÃ?CS ANGÉLA; Láng Orsolya; MEZO DIÃ?NA 权利人:EOETVOES LORAND TUDOMANYEGYETEM; SEMMELWEIS EGYETEM 摘要:The present invention relates to compounds of formula (I) (I) or pharmaceutically acceptable salts, and stereoisomers thereof, including enantiomers, racemic mixtures, mixtures of enantiomers, or combinations thereof, which are applicable for use in treating cancer diseases. The present invention further relates to a pharmaceutical composition comprising the above compounds.
专利号:WO-2023122754-A1 优先权日:2021-12-23 标 题 :Processes and intermediates for preparing gb13, gb22 and himgaline 发明人:LANDWEHR ELEANOR; SHENVI RYAN; BAKER MEGHAN; OGUMA TAKUYA 权利人:SCRIPPS RESEARCH INST 摘要:Provided herein are processes for the streamlined synthesis of Galbulimima alkaloids, such as himbadine, isolated from Galbulimima belgraveana and G. baccatta, trees endemic to the rainforests of Northern Australia and Papua New Guinea, as well as analogs thereof, such as GB13, GB16, GB22, and himgaline, and further including intermediates useful in the synthesis of these and related compounds.
专利号:US-10253004-B2 优先权日:2017-01-26 标 题:Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof 发明人:ECKHARDT MATTHIAS; WAGNER HOLGER; PETERS STEFAN 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of formula I, n nwherein the groups R, R 1 , R 2 , R 3 , m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-6004965-A 优先权日:1994-12-20 标题 :Sulfonamides 发明人:BREU VOLKER; BURRI KASPAR; CASSAL JEAN-MARIE; CLOZEL MARTINE; HIRTH GEORGES; LOEFFLER BERND-MICHAEL; MUELLER MARCEL; NEIDHART WERNER; RAMUZ HENRI 权利人:HOFFMANN LA ROCHE 摘要:Compounds of the formula: ##STR1## where A, B, R 1 -R 8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
专利号:SU-1456426-A1 优先权日:1987-07-03 标 题:Derivatives of dibenzoxazols as monomers for synthesis of soluble heat-resistant polybenzimidazolbenzoxasols
专利号:EP-4192467-A1 优先权日:2020-08-06 标题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity
[参考文献]: Luo Mei, Et Al. Modular Synthesis Of Oxazolines And Their Derivatives. J Comb Chem. 2009 Mar 9;11(2):220-7.
合成参考文献
摘要:Bertus, P.; Boeda, F.; Pearson-Long, M. S. M., Science of Synthesis Knowledge Updates, (2012) 1, 41. 摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 374. 摘要:Yan, G.; Zhang, Y.; Wang, Jianbo, Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 524. 摘要:Asano, Y., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 263. 摘要:Ouali, A.; Taillefer, M., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 97.