CAS: 124150-87-4; (R)-Tert-Butyldimethyl(Oxiran-2-Ylmethoxy)Silane

相似化合物

123237-62-7 57044-25-4 60456-23-7

上下游产品

Allyloxy-tert-butyl-dimethyl-silane oxiranyl-methanol tert-butyldimethylsilyl chloride 1H-imidazole(2S,4R)-4-Benzenesulfonyl-1-(tert-butyl-dimethyl-silanyloxy)-4-cyclopent-1-enyl-butan-2-ol (2R,4R)-4-Benzenesulfonyl-1-(tert-butyl-dimethyl-silanyloxy)-4-cyclopent-1-enyl-butan-2-ol 1-((tert-butyldimethylsilyl)oxy)-3-phenylpropan-2-ol 1-(tert-butyl-dimethylsilyloxy)-4-phenylbutan-2-ol

叔丁基二甲基甲硅烷基缩水甘油醚置于(S,S)-(+)-N,N'-Bis(3,5-Di-Tert-Butylsalicylidene)-1,2-Cyclohexanediaminocobalt(II),溶剂黄146体系中,用 四氢呋喃,水 用作溶剂,化学反应 21.0H,以50%的收率获得(R)-T-叔丁基二甲基硅基缩水甘油醚
参考文献:新型tlr2激动剂的合成和评价,可作为癌症疫苗的潜在佐剂.
标题:新型tlr2激动剂的合成和评价,可作为癌症疫苗的潜在佐剂.
摘要:与更传统的治疗方式相比,癌症免疫疗法由于其潜在的特异性和缺乏不良副作用而受到越来越多的关注.Toll样受体2(tlr2)激动剂是脂肽,具有s-[2,3-双(棕榈酰氧基)丙基]-1-半胱氨酸(pam 2 Cys)基序,并表现出强大的免疫刺激作用.这些激动剂提供了一种提供"危险信号"的方式,以激活针对肿瘤抗原的免疫系统.因此,在寻找潜在的癌症免疫刺激剂方面,Tlr2激动剂的开发具有吸引力.Pam 2的现有sar研究带有tlr2的半胱氨酸表明,对活性的结构要求在大多数情况下是非常难以忍受的.我们研发了立体化学的重要性,N末端酰化的影响以及pam 2 Cys结合的脂肽中两个酯官能团之间对tlr2活性的同源性.的[r非对映体是显著比更有效小号非对映体和ñ末端修饰通常降低tlr2活性.最显着地,同源性产生了对含有天然pam 2 Cys的构建体具有相对活性的类似物.
Doi:10.1021/acs.Jmedchem.9B01044

专利信息

专利号:US-9328066-B2
优先权日:2011-05-27
标 题 :Chiral synthesis of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides
发明人：FEY PETER; MAYER AGATHE CHRISTINE
权利人:FEY PETER; MAYER AGATHE CHRISTINE; BAYER IP GMBH
摘要:The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.

专利号:CA-2837162-A1
优先权日:2011-05-27
标 题:Chiral synthesis of n-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides

专利号:EP-2714652-A1
优先权日:2011-05-27
标题:Chiral synthesis of n-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides

专利号:US-2014155637-A1
优先权日:2011-05-27
标题 :Chiral synthesis of n--1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides

专利号:IL-228911-A
优先权日:2011-05-27
标 题:Cyralic synthesis of} -n-4,3-diplooro-2 [(2-fluoro-4-iodophenyl) amino] -6-methoxyphenyl} -1- [3,2-dihydroxy-profile] cyclopropanesulfonamides

专利号:CA-2837162-C
优先权日:2011-05-27
标题:Chiral synthesis of n-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides