Article(id=1322246436679430592, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1595433600000, acceptedDateStr=2020-07-23, onlineDate=1793177716655, onlineDateStr=2026-10-28, pubDate=1623686400000, pubDateStr=2021-06-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1793177716655, onlineIssueDateStr=2026-10-28, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1793177716655, creator=13701087609, updateTime=1793177716655, updator=13701087609, issue=Issue{id=1322246381633389353, tenantId=1146029695717560320, journalId=1235980733773295621, year='2021', volume='30', issue='11', pageStart='961', pageEnd='1056', issueExtLink='null', onlineDate='null', pubDate='1623686400000', pubDateStr='2021-06-15', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1793177703531, creator='13701087609', updateTime=1793178125547, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1322248152208486593, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1322248152212680898, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=1008, endPage=1013, ext={EN=ArticleExt(id=1322246437191135681, articleId=1322246436679430592, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Recent development of synthesis of key intermediate of minodronic acid, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=

Minodronic acid is a third-generation nitrogen-containing heterocyclic bisphosphonate drug mainly used for the treatment of osteoporosis and hypercalcemia caused by osteoporosis and malignant tumors. Through summary of the existing literature, it was found that the research on the synthesis of minodronic acid is mainly concentrated on the synthesis of the key intermediate 2-(imidazo[1,2-a]pyridin-3-yl) acetic acid, and the preparation of this intermediate is mainly based on the fact that the 3-position of the imidazo[1,2-a]pyridine's structure contains a substituent group which is susceptible to functional group conversion. The synthesis technology of minodronic acid by phosphorylation of this intermediate is relatively simple. The synthesis strategy of the key intermediate 2-(imidazo[1,2-a]pyridin-3-yl) acetic acid is reviewed in this article.

, authors=Yong-yu OU1, 2, Ran-ran ZHU1, Tian-en TIAN1, Jian-yao WANG1, Dong CHEN1, Chang-shan SUN2, authorsList=Yong-yu OU, Ran-ran ZHU, Tian-en TIAN, Jian-yao WANG, Dong CHEN, Chang-shan SUN, authorCompany=null, correspAuthors=Chang-shan SUN, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1322246437925138882, articleId=1322246436679430592, tenantId=1146029695717560320, journalId=1235980733773295621, language=CN, title=米诺膦酸关键中间体合成工艺研究进展, columnId=1236330553964810454, journalTitle=中国新药杂志, columnName=综述, runingTitle=null, highlight=null, articleAbstract=

米诺膦酸作为第三代含氮芳杂环双膦酸盐类药物,主要用于治疗骨质疏松症以及由骨质疏松症和恶性肿瘤引起的高钙血症。通过对已有文献资料的归纳总结发现,米诺膦酸的合成研究主要集中在关键中间体2-(咪唑并[1,2-a]吡啶-3-基)乙酸的合成,而该中间体的制备较大程度上是来源于咪唑并[1,2-a]吡啶母核结构的3位含有易于进行官能团转化的取代基。而由该中间体通过磷酸化合成米诺膦酸的合成技术较为单一,因此本文主要针对米诺磷酸关键中间体2-(咪唑并[1,2-a]吡啶-3-基)乙酸的合成策略进行综述。

, authors=欧永玉1, 2, 朱冉冉1, 田天恩1, 王建耀1, 陈东1, 孙长山2, authorsList=欧永玉, 朱冉冉, 田天恩, 王建耀, 陈东, 孙长山, authorCompany=null, correspAuthors=孙长山, authorNote=

欧永玉,男,硕士,研究方向:从事仿制药研发工作。联系电话:(010)80728999,E-mail:。

, correspAuthorsNote=
孙长山,男,教授,研究方向:新技术与新剂型、新药研究与开发。E-mail:。
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欧永玉,男,硕士,研究方向:从事仿制药研发工作。联系电话:(010)80728999,E-mail:。

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欧永玉,男,硕士,研究方向:从事仿制药研发工作。联系电话:(010)80728999,E-mail:。

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米诺膦酸关键中间体合成工艺研究进展
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欧永玉 1, 2 , 朱冉冉 1 , 田天恩 1 , 王建耀 1 , 陈东 1 , 孙长山 2
中国新药杂志 | 综述 2021,30(11): 1008-1013
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中国新药杂志 |综述 2021 , 30 (11) : 1008 -1013
米诺膦酸关键中间体合成工艺研究进展
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欧永玉,男,硕士,研究方向:从事仿制药研发工作。联系电话:(010)80728999,E-mail:。

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欧永玉,男,硕士,研究方向:从事仿制药研发工作。联系电话:(010)80728999,E-mail:。

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欧永玉1, 2 , 朱冉冉1, 田天恩1, 王建耀1, 陈东1, 孙长山2
作者信息
  • 1扬子江药业集团北京海燕药业有限公司,北京 102206
  • 2沈阳药科大学,沈阳 110016
通讯作者:
孙长山,男,教授,研究方向:新技术与新剂型、新药研究与开发。E-mail:。
作者简介:

欧永玉,男,硕士,研究方向:从事仿制药研发工作。联系电话:(010)80728999,E-mail:。

Recent development of synthesis of key intermediate of minodronic acid
Yong-yu OU1, 2 , Ran-ran ZHU1, Tian-en TIAN1, Jian-yao WANG1, Dong CHEN1, Chang-shan SUN2
Affiliations
  • 1Yangtze River Pharmaceutical Group, Beijing Haiyan Pharmaceutical Co., Ltd., Beijing 102206, China
  • 2Shenyang Pharmaceutical University, Shenyang 110016, China
出版时间: 2021-06-15
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米诺膦酸作为第三代含氮芳杂环双膦酸盐类药物,主要用于治疗骨质疏松症以及由骨质疏松症和恶性肿瘤引起的高钙血症。通过对已有文献资料的归纳总结发现,米诺膦酸的合成研究主要集中在关键中间体2-(咪唑并[1,2-a]吡啶-3-基)乙酸的合成,而该中间体的制备较大程度上是来源于咪唑并[1,2-a]吡啶母核结构的3位含有易于进行官能团转化的取代基。而由该中间体通过磷酸化合成米诺膦酸的合成技术较为单一,因此本文主要针对米诺磷酸关键中间体2-(咪唑并[1,2-a]吡啶-3-基)乙酸的合成策略进行综述。

米诺膦酸  /  关键中间体  /  骨质疏松症  /  磷酸化  /  合成策略

Minodronic acid is a third-generation nitrogen-containing heterocyclic bisphosphonate drug mainly used for the treatment of osteoporosis and hypercalcemia caused by osteoporosis and malignant tumors. Through summary of the existing literature, it was found that the research on the synthesis of minodronic acid is mainly concentrated on the synthesis of the key intermediate 2-(imidazo[1,2-a]pyridin-3-yl) acetic acid, and the preparation of this intermediate is mainly based on the fact that the 3-position of the imidazo[1,2-a]pyridine's structure contains a substituent group which is susceptible to functional group conversion. The synthesis technology of minodronic acid by phosphorylation of this intermediate is relatively simple. The synthesis strategy of the key intermediate 2-(imidazo[1,2-a]pyridin-3-yl) acetic acid is reviewed in this article.

minodronic acid  /  key intermediate  /  osteoporosis  /  phosphorylation  /  synthesis strategy
欧永玉, 朱冉冉, 田天恩, 王建耀, 陈东, 孙长山. 米诺膦酸关键中间体合成工艺研究进展. 中国新药杂志, 2021 , 30 (11) : 1008 -1013 .
Yong-yu OU, Ran-ran ZHU, Tian-en TIAN, Jian-yao WANG, Dong CHEN, Chang-shan SUN. Recent development of synthesis of key intermediate of minodronic acid[J]. Chinese Journal of New Drugs, 2021 , 30 (11) : 1008 -1013 .

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2021年第30卷第11期
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  • 首发时间:2026-10-28
  • 出版时间:2021-06-15
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    1扬子江药业集团北京海燕药业有限公司,北京 102206
    2沈阳药科大学,沈阳 110016

通讯作者:

孙长山,男,教授,研究方向:新技术与新剂型、新药研究与开发。E-mail:。
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2种不同金属材料的力学参数
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species
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Percentage of
total species (%)
属
Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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