Synthesis of <sup>3</sup>H and <sup>14</sup>C labelled changrolin

Xin Zhang; Yuewen Bao; Ruiqin Ding

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Synthesis of ³H and ¹⁴C labelled changrolin

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- Synthesis of ³H and ¹⁴C labelled changrolin
- Nuclear Techniques Vol. 11, Issue 5, (1988)
- 作者机构：
  
  中国科学院上海药物研究所
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Received：23 March 1987，
  
  Published：1988-05
- 稿件说明：
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Xin Zhang, Yuewen Bao, Ruiqin Ding. Synthesis of ³H and ¹⁴C labelled changrolin[J]. Nuclear techniques, 1988, 11(5): 29-31.
DOI：

Xin Zhang, Yuewen Bao, Ruiqin Ding. Synthesis of ³H and ¹⁴C labelled changrolin[J]. Nuclear techniques, 1988, 11(5): 29-31. DOI：

摘要

本文用合成方法制备了抗心律不齐新药常咯啉的三种不同位置

H和

C的标记化合物。以5-溴邻氨基苯甲酸按Scheme 1经5步反应得6-溴代常咯啉（Ⅵ），Ⅵ用氚经催化脱卤得〔6-

H〕常咯啉（Ⅰ）用〔

C〕甲酸制成〔

C〕甲酰胺，按Scheme 1经二步反应得〔2

C〕5-氯代喹唑啉（V

R＝H）再按Scheme2即得〔2-

C〕常咯啉（Ⅱ）。以〔

C〕甲醛为原料按Scheme1的最后一步可直接制得（甲撑-

C〕常咯啉（Ⅲ）

Abstract

In this paper 3 kinds of 〔

C〕 and 〔

H〕 changrolin labelled at different positions (Ⅰ

Ⅱ

Ⅲ) were prepared. The synthesis of I was illustrated in Scheme 1. Heating 5-bromoanthranilic acid with formamide yielded Ⅳ

which on heating with POCl

gave V. Condensation of V with 4-aminophenol and then subjected to Mannich reaction produced 6-bromochangrolin (Ⅵ)

Catalytic dehalogenation of Ⅵ with tritium gas gave I. The synthesis of Ⅱ was started from (

C) formamide and anthranilic acid. Labelled 4-chloroquine obtained was condensed with Mannich base (Ⅶ) directly (Scheme 2). Ⅲwas prepared by 1 step with (

C) formaldehyde (Scheme 1).

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references

李良泉等，中国科学，（ 1979 ）， 723 。

常咯啉临床协作组，中华医学杂志， 58 （ 1987 ）， 84 。

孙存济等，药学学报， 16 （ 1981 ）， 8 ： 564 。

D. M. Stout et al ., J. Med, Cham ., 26 ( 1982 ), 808 ； 27 ( 1984 ), 1347 .

A. B. Sen and P. R. Singh , J. Indian, Chem. Soc ., 36 ( 1959 ), 787 .

F. Weygand et al ., Angew. Chem ., 64 ( 1954 ), 174 .

A. Murray et al ; Organic Synthesis with Isotopes Part I. Interscience Publishers Inc. , New York , 1958 , p 607 .

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Synthesis of 3H and 14C labelled changrolin

DOI：

摘要

Abstract

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Synthesis of ³H and ¹⁴C labelled changrolin