CAS: 106946-74-1; Tert-Butyl ((2S,3S)-1-Hydroxy-3-Methylpentan-2-yl)Carbamate

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N-(tert-butyloxycarbonyl)-L-isoleucine N-(tert-butoxycarbonyl)isoleucine methyl ester 15H27NO6C15H27NO6 L-isoleucineN-(t-butoxycarbonyl)-isoleucine aldehyde (S) 1-hydroxy-O-(p-toluenesulfonyl)-2-amino-N-(tert-butyloxycarbonyl)-3-methyl-pentane imidazol-4-yl)-1-oxopentyl>amino>methyl>-2-methylbutyl>-2-(1-methylethyl)-5-amino-, >-L-idonamide, 6-cyclohexyl-2,5,6-trideoxy-N-1-5-(hexahydro-2-oxo-1H-thieno3,4-dimidazol-4-yl)-1-oxopentylaminomethyl-2-methylbutyl-2-(1-methylethyl)-5-amino-, 3aS-3aα,4β(1R*,2R*),6aα- amino>ethyl>-2,2-dimethyl-α-(1-methylethyl)-N-imidazol-4-yl)-1-oxopentyl>-, >-1,3-dioxolane-4-acetamide, 5-2-cyclohexyl-1-(1,1-dimethylethoxy)carbonylaminoethyl-2,2-dimethyl-α-(1-methylethyl)-N-5-(hexahydro-2-oxo-1H-thieno3,4-dimidazol-4-yl)-1-oxopentyl-, 3aS-3aα,4β(1R*,2R*,3S*,4S*),6aα-

L-异亮氨酸置于sodium Tetrahydroborate,碘体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应 17.5H,反应生成N-Boc-L-异亮氨醇
参考文献:四氢喹啉衍生的大环工具箱:斑马鱼测定中抗血管生成剂的发现.
标题:四氢喹啉衍生的大环工具箱:斑马鱼测定中抗血管生成剂的发现.
摘要:开发了一种将大环结合到特权子结构(即四氢喹啉骨架)上的新颖方法.大环骨架中氨基酸衍生部分的存在为调节手性侧链的性质提供了机会.此外,在斑马鱼筛选中的评估确定了三个活性小分子(2.5B,3.2D和4.2)为2.5μm的抗血管生成剂.
Doi:10.1021/ml400026N

专利信息

专利号:US-5378690-A
优先权日:1986-12-19
标题 :New renin-inhibitory oligopeptides, their preparation and their use
发明人：MORISAWA YASUHIRO; KATAOKA MITSURU; YABE YUICHIRO; IIJIMA YASUTERU; TAKAHAGI HIDEKUNI; KOIKE HIROYUKI; KOKUBU TATSUO; HIWADA KUNIO
权利人:SANKYO CO
摘要:Oligopeptides of formula (I): (I) where R1-R5 are various organic groups, and A represents a group of formula -NH- or -(CH2)n-, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.