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【结 构 式】

【分子编号】32026

【品名】1-chloro-4-iodobutane

【CA登记号】10297-05-9

【 分 子 式 】C4H8ClI

【 分 子 量 】218.46469

【元素组成】C 21.99% H 3.69% Cl 16.23% I 58.09%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(XIV)

The reaction of the labeled acylated (-)-bornane-10,2-sultam (XI) with benzophenone imine (XII) gives the glycylsultam derivative (XIII), which is alkylated with 4-iodobutyl chloride (XIV) by means of butyllithium and DMPU in THF yielding intermediate (XV). The selective hydrolysis of (XV) with HCl affords the omega-chloro-L-norleucine derivative (XVI), which is cyclized by means of tetrabutylammonium fluoride and DIEA in hot acetonitrile giving the (2S)-piperidyl derivative (XVII). Finally, this compound is hydrolyzed with LiOH in THF/water to the labeled intermediate (II).

1 Moenius, T.; et al.; C-14 labelling of NVP RAD001 - A new rapamycin derivative. J Label Compd Radiopharm 1999, 42, 1, 29.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(II) 17380 (2S)hexahydro-2-pyridinecarboxylic acid; (S)-pipecolic acid 3105-95-1 C6H11NO2 详情 详情
(II) 45303 (2S)-2-piperidinecarboxylic acid C6H11NO2 详情 详情
(XI) 32030 (1R,5R)-4-(2-bromoacetyl)-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C12H18BrNO3S 详情 详情
(XI) 45315 (1R,5R)-4-(2-bromoacetyl)-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C12H18BrNO3S 详情 详情
(XII) 32024 diphenylmethanimine 1013-88-3 C13H11N 详情 详情
(XIII) 32025 (1R,5R)-4-[2-[(dibenzylene)amino]acetyl]-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C25H28N2O3S 详情 详情
(XIII) 45311 (1R,5R)-4-[2-[(dibenzylene)amino]acetyl]-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C25H28N2O3S 详情 详情
(XIV) 32026 1-chloro-4-iodobutane 10297-05-9 C4H8ClI 详情 详情
(XV) 32027 (1R,5R)-4-[(2S)-6-chloro-2-[(dibenzylene)amino]hexanoyl]-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C29H35ClN2O3S 详情 详情
(XV) 45312 (1R,5R)-4-[(2S)-6-chloro-2-[(dibenzylene)amino]hexanoyl]-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C29H35ClN2O3S 详情 详情
(XVI) 32028 (1R,5R)-4-[(2S)-2-amino-6-chlorohexanoyl]-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C16H27ClN2O3S 详情 详情
(XVI) 45313 (1R,5R)-4-[(2S)-2-amino-6-chlorohexanoyl]-10,10-dimethyl-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C16H27ClN2O3S 详情 详情
(XVII) 32029 (1R,5R)-10,10-dimethyl-4-[(2S)piperidinylcarbonyl]-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C16H26N2O3S 详情 详情
(XVII) 45314 (1R,5R)-10,10-dimethyl-4-[(2S)piperidinylcarbonyl]-3lambda(6)-thia-4-azatricyclo[5.2.1.0(1,5)]decane-3,3-dione C16H26N2O3S 详情 详情
Extended Information