CAS: 95530-58-8; (R)-4-Isopropyloxazolidin-2-One

相似化合物

103723-70-2 17016-83-0 54705-42-9

上下游产品

phosgene valinol 4-methoxy-1,3-oxazolidin-2-one isopropylmagnesium bromide (4S)-4-isopropyl-1,3-oxazolidin-2-one valinol

D-缬氨酸置于sodium Tetrahydroborate,碘,Potassium Carbonate体系中,用 四氢呋喃 作为反应溶剂,化学反应 18.0H,反应生成 (R)-(+)-4-异丙基-2-恶唑啉酮
参考文献:Synthesis Of Salicylic Acid-Based 1,3,4-Oxadiazole Derivatives Coupled With Chiral Oxazolidinones: Novel Hybrid Heterocycles As Antitumor Agents
标题:Synthesis Of Salicylic Acid-Based 1,3,4-Oxadiazole Derivatives Coupled With Chiral Oxazolidinones: Novel Hybrid Heterocycles As Antitumor Agents
摘要:一系列新颖的水杨酸基1,3,4-噁二唑衍生物与手性噁唑烷酮结合,被合成用于筛选其对五种人癌细胞系的体外抗肿瘤活性.其中一些化合物显示出非常好的抗肿瘤活性,Ic50值范围在31.19-57.21 µm之间.在测试的化合物中,11,15,19,23,24和34表现出对所有细胞系的广谱抗肿瘤活性.特别是化合物19显示出显著的抗肿瘤活性,Ic50 = 31.19-41.87 µm.a431细胞系对所有研究化合物最为敏感,其次是hela,Mcf-7,A549和hepg2.新合成化合物的结构通过ir,1H NMR,13C NMR和hrms光谱数据得到确认.
DOI:10.2174/1570180811666140627004607

专利信息

专利号:WO-2017033128-A1
优先权日:2015-08-25
标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors
发明人：HOOK DAVID; KU JIE; ZHOU JIANGUANG
权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG
摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.

专利号:US-5554788-A
优先权日:1992-10-01
标 题 :Process for the stereoselective synthesis of 3-substituted 2-thiomethylpropionic acids
发明人：HOLLA WOLFGANG; KAMMERMEIER BERNHARD; BECK GERHARD
权利人:HOECHST AG
摘要:PCT No. PCT/EP93/02673 Sec. 371 Date May 15, 1995 Sec. 102(e) Date May 15, 1995 PCT Filed Sep. 30, 1993 PCT Pub. No. WO94/00789 PCT Pub. Date Apr. 14, 1994Process for the stereoselective synthesis of 3-substituted 2-thiomethylpropionic acids Compounds of the formula I I in which R1 and R2 are as defined can be prepared stereoselectively by reaction of acrylic acid or derivatives thereof or propionic acid or derivatives thereof with a chiral auxiliary, reaction with a mercaptan, stereoselective alkylation and subsequent hydrolysis and oxidation.

专利号:US-10611739-B2
优先权日:2016-08-16
标题:Process for preparation of lactone derivatives and intermediates thereof
发明人：CHEN PING; PENG SHAOPING; LI YINQIANG; LI DAFENG; DONG XUEJUN
权利人:PHARMARESOURCES SHANGHAI CO LTD
摘要:A novel process for the preparation of lactone derivatives, and intermediates thereof is described. The lactone derivatives are important precursors for the synthesis of anti-hepatitis C virus agents, including sofosbuvir.

专利号:US-8853228-B2
优先权日:2007-06-04
标 题:Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase
发明人：ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE
权利人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE; UNIV CONNECTICUT
摘要:The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.

专利号:US-8426432-B2
优先权日:2007-06-04
标 题 :Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties
发明人：ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO
权利人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO; UNIV CONNECTICUT
摘要:The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.

专利号:WO-9407849-A1
优先权日:1992-10-01
标题:Process for the stereoselective synthesis of 3-substituted 2-thiomethyl propionic acids