Title:
METHOD FOR PREPARING NATURAL ACTIVE POLYPEPTIDE TUBULYSIN U
Document Type and Number:
WIPO Patent Application WO/2021/227512
Kind Code:
A1
Abstract:
Provided is a novel method for preparing natural active polypeptide Tubulysin U, the synthetic route of the preparation method satisfies the Green Chemistry standard and utilizes as much as possible renewable and recyclable resources, the reagents used have relatively low toxicity, and the reaction produces little environmental pollution after being treated. In particular, the preparation method has a relatively high overall yield, good stereoselectivity, convenient experimental operations, mild reaction conditions, simple separation and purification, and can be used for large-scale preparation.
Inventors:
WU ZHENGZHI (CN)
LONG BOHUA (CN)
LI YINGHONG (CN)
LIU JIEREN (CN)
LI LIMIN (CN)
LONG BOHUA (CN)
LI YINGHONG (CN)
LIU JIEREN (CN)
LI LIMIN (CN)
Application Number:
PCT/CN2020/139779
Publication Date:
November 18, 2021
Filing Date:
December 27, 2020
Export Citation:
Assignee:
SHENZHEN INST GERIATRICS (CN)
WU ZHENGZHI (CN)
WU ZHENGZHI (CN)
International Classes:
C07K5/078; C07K1/02; C07K1/06; C07K1/10
Domestic Patent References:
| WO2010034724A1 | 2010-04-01 |
Foreign References:
| CN111647040A | 2020-09-11 | |||
| CN110684044A | 2020-01-14 | |||
| CN104072578A | 2014-10-01 | |||
| EP2292639A1 | 2011-03-09 |
Other References:
LONG BOHUA, TAO CHENG, LI YINGHONG, ZENG XIAOBIN, CAO MEIQUN, WU ZHENGZHI: "Total synthesis of tubulysin U and N 14 -desacetoxytubulysin H", ORGANIC & BIOMOLECULAR CHEMISTRY, ROYAL SOCIETY OF CHEMISTRY, vol. 18, no. 28, 22 July 2020 (2020-07-22), pages 5349 - 5353, XP055866949, ISSN: 1477-0520, DOI: 10.1039/D0OB01109F
WEI XIAOYUN: "Study on the Total Synthesis of Bioactive Marine Natural Products of Hapalosin and Tubulysin V", CHINESE MASTER’S THESES FULL-TEXT DATABASE, ENGINEERING SCIENCE AND TECHNOLOGY I, no. 7, 15 July 2014 (2014-07-15), XP055866960
PETER WIPF, TAKESHI TAKADA, MICHAEL J. RISHEL: "Synthesis of the Tubuvaline-Tubuphenylalanine (Tuv-Tup) Fragment of Tubulysin", ORGANIC LETTERS, AMERICAN CHEMICAL SOCIETY, US, vol. 6, no. 22, 1 October 2004 (2004-10-01), US , pages 4057 - 4060, XP055532591, ISSN: 1523-7060, DOI: 10.1021/ol048252i
SHAO MINGSHA: "The Studies on the Structural Modification of Pretubulysin and Antitumor Activity in vitro", MEDICINE AND HEALTH SCIENCES, CHINESE MASTER’S THESES FULL-TEXT DATABASE, no. 9, 15 September 2019 (2019-09-15), XP055866953
SHIBUE TAKU, HIRAI TOSHIHIRO, OKAMOTO IWAO, MORITA NOBUYOSHI, MASU HYUMA, AZUMAYA ISAO, TAMURA OSAMU: "Total Syntheses of Tubulysins", CHEMISTRY - A EUROPEAN JOURNAL, JOHN WILEY & SONS, INC, vol. 16, no. 38, 11 October 2010 (2010-10-11), pages 11678 - 11688, XP055866951, ISSN: 0947-6539, DOI: 10.1002/chem.201000963
WEI XIAOYUN: "Study on the Total Synthesis of Bioactive Marine Natural Products of Hapalosin and Tubulysin V", CHINESE MASTER’S THESES FULL-TEXT DATABASE, ENGINEERING SCIENCE AND TECHNOLOGY I, no. 7, 15 July 2014 (2014-07-15), XP055866960
PETER WIPF, TAKESHI TAKADA, MICHAEL J. RISHEL: "Synthesis of the Tubuvaline-Tubuphenylalanine (Tuv-Tup) Fragment of Tubulysin", ORGANIC LETTERS, AMERICAN CHEMICAL SOCIETY, US, vol. 6, no. 22, 1 October 2004 (2004-10-01), US , pages 4057 - 4060, XP055532591, ISSN: 1523-7060, DOI: 10.1021/ol048252i
SHAO MINGSHA: "The Studies on the Structural Modification of Pretubulysin and Antitumor Activity in vitro", MEDICINE AND HEALTH SCIENCES, CHINESE MASTER’S THESES FULL-TEXT DATABASE, no. 9, 15 September 2019 (2019-09-15), XP055866953
SHIBUE TAKU, HIRAI TOSHIHIRO, OKAMOTO IWAO, MORITA NOBUYOSHI, MASU HYUMA, AZUMAYA ISAO, TAMURA OSAMU: "Total Syntheses of Tubulysins", CHEMISTRY - A EUROPEAN JOURNAL, JOHN WILEY & SONS, INC, vol. 16, no. 38, 11 October 2010 (2010-10-11), pages 11678 - 11688, XP055866951, ISSN: 0947-6539, DOI: 10.1002/chem.201000963
Attorney, Agent or Firm:
SHINY INTELLECTUAL PROPERTY FIRM (CN)
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