| SYNTHESIS OF α-AMINO-β-(4-IMIDAZOLYL)-ETHYLPHOSPHONIC ACID,THE PHOSPHONOISOSTERE OF HISTIDINE |
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| 作者姓名： | Yuan Liu WU Max TISHLER |
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| 作者单位： | a Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050;b Hall-Atwater Laboratories, Department of Chemistry, Wesleyan University, Middletown, Conn. 06457, USA |
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| 摘 要： | A short synthesis starting from 4-imidazolylmethanol(2)was developedfor the phosphonoisostere of histidine,-amino-β-(4-imidazolyl)-ethylphosphosphonic acid,His(P)(1).The synthesis features Wittig-Hornerreaction of aldehyde(4)with diphosphonate(5)followed by selectivedetritylation with 50% formic acid.
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SYNTHESIS OF α-AMINO-β-(4-IMIDAZOLYL)-ETHYLPHOSPHONIC ACID,THE PHOSPHONOISOSTERE OF HISTIDINE |
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| Yuan Liu WU,Max TISHLER.SYNTHESIS OF α-AMINO-β-(4-IMIDAZOLYL)-ETHYLPHOSPHONIC ACID,THE PHOSPHONOISOSTERE OF HISTIDINE[J].Chinese Chemical Letters,1991,2(2):95-98. |
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| Authors: | Yuan Liu WU Max TISHLER |
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| Institution: | a Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050;b Hall-Atwater Laboratories, Department of Chemistry, Wesleyan University, Middletown, Conn. 06457, USA |
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| Abstract: | A short synthesis starting from 4-imidazolylmethanol (2) was developed for the phosphonoisostere of histidine, α-amino-β-(4-imidazolyl)-ethylphosphosphonic acid, His (P) (1). The synthesis features Wittig-Horner reaction of aldehyde (4) with diphosphonate (5) followed by selective detritylation with 50% formic acid. |
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