公开(公告)号：KR100287365B1

公开(公告)日：2001-04-16

申请号：KR1019990001314

申请日：1999-01-18

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  이기수 ,  변종수 ,  이명철 ,  정준기 ,  이동수 ,  정재민

IPC: C07D207/00

Abstract: 본발명에서는 NS리간드가결합된라클로프라이드유도체및 이의제조방법을제공하여도파민 D2의수용체영상용화합물로서적합한성질인방사화학적으로가장최적의물리적조건(제조용이성, 반감기, 방사능세기, 구매용이성)을가지는화합물에관한것이다.

公开(公告)号：KR1020000020032A

公开(公告)日：2000-04-15

申请号：KR1019980038442

申请日：1998-09-17

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  이기수 ,  진경용 ,  이명철 ,  정준기 ,  이동수 ,  정재민

IPC: C07C321/04

Abstract: PURPOSE: Title derivatives useful as radioactive pharmaceuticals are prepared which can extend a residual time in heart, and minimize a radioactive disturbance. CONSTITUTION: 1,12-Dodecane diol is alcohol-substituted by bromic acid to give 12-bromo-dodecane-1-ol, and protected by tetrahydropyrane. Obtained dodecane, 2-ethyl-4,4-dimethyl-2-oxazoline and n-butyl lithium are reacted to give 2(R/S)-(4,4-dimethyl-2-oxazoline-2-yl)-12-tetrahydropyranyl oxy-tetradecane, and esterified with sulfuric acid to give ethyl-2(R/S)-methyl-12-hydroxytetradecaneate. Obtained tetradecaneate is protected to give ethyl-2(R/S)-methyl-14-tetra butyl dimethyl silyloxy-tetradecaneate, followed by reduction with lithium aluminum hydride to give 2(R/S)-methyl-14-t-butyl dimethyl silyloxy-tetradecane-1-ol, tosylated by tosyl chloride, and to give 3(R/S)-methyl-15-t-butyl dimethyl silyloxy-pentadecane-nitrile by substituting with sodium cyanide. Obtained nitride is treated with 1N-hydrochloric acid, hydrolyzed and mesylated to give 16-methane sulfonyl-3-methyl-pentadecanic acid. The pentadecanic acid is brominated, followed by reaction of thiourea and NaOH to give 15-mercapto-3-methyl-pentadecanic acid(formula 1).

Abstract translation: 目的：制备用作放射性药物的标题衍生物，其可以延长心脏中的残留时间，并使放射性干扰最小化。 构成：1,12-十二烷二醇被溴酸醇取代，得到12-溴 - 十二烷-1-醇，并用四氢吡喃保护。 获得的十二烷，2-乙基-4,4-二甲基-2-恶唑啉和正丁基锂反应，得到2（R / S） - （4,4-二甲基-2-恶唑啉-2-基） 四氢呋喃基氧基十四烷，并用硫酸酯化，得到乙基-2（R / S） - 甲基-12-羟基十四烷酸酯。 得到的十四烷酸乙酯得到乙基-2（R / S） - 甲基-14-四丁基二甲基甲硅烷氧基 - 十四烷酸酯，然后用氢化铝锂还原，得到2（R / S） - 甲基-14-叔丁基二甲基 甲硅烷氧基 - 十四烷-1-醇，用甲苯磺酰氯甲磺酰化，并用氰化钠代替得到3（R / S） - 甲基-15-叔丁基二甲基甲硅烷氧基 - 十五烷腈。 得到的氮化物用1N盐酸处理，水解和甲磺酰化得到16-甲磺酰基-3-甲基 - 十五烷酸。 将十五烷酸溴化，随后用硫脲和NaOH反应，得到15-巯基-3-甲基 - 十五烷酸（式1）。