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Title:
COMPOSITIONS AND METHODS FOR CONSTRUCTING CONJUGATES
Document Type and Number:
WIPO Patent Application WO/2024/041521
Kind Code:
A1
Abstract:
Disclosed are methods for constructing conjugates. An amine-containing component and a thiol-containing component, in comparable mole ratios, react with an ortho-phthalaldehyde in one step, to generate a conjugate bearing a substituted or an unsubstituted 1-thio-isoindole structure in the presence of an additive. The method provides a platform for the efficient and practical constructions of bioactive modular motifs.

Inventors:
LI XUECHEN (CN)
CHEUNG HEY PUI (CN)
Application Number:
PCT/CN2023/114213
Publication Date:
February 29, 2024
Filing Date:
August 22, 2023
Export Citation:
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Assignee:
UNIV HONG KONG (CN)
International Classes:
C07C47/544; C07D209/44; C07K1/04
Domestic Patent References:
WO2020103891A12020-05-28
Foreign References:
CN115043899A2022-09-13
CN104877982A2015-09-02
CN113087653A2021-07-09
Other References:
CHEUNG CARINA HEY PUI, CHONG TIN HANG, WEI TONGYAO, LIU HAN, LI XUECHEN: "Guanidine Additive Enabled Intermolecular ortho‐ Phthalaldehyde‐Amine‐Thiol Three‐Component Reactions for Modular Constructions", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, VERLAG CHEMIE, HOBOKEN, USA, vol. 62, no. 10, 1 March 2023 (2023-03-01), Hoboken, USA, pages , e202217150, XP093142249, ISSN: 1433-7851, DOI: 10.1002/anie.202217150
NIE QIGUI, FANG XIANFU, LIU CHANGYANG, ZHANG GONG, FAN XIAOHONG, LI YANGFENG, LI YIZHOU: "DNA-Compatible ortho -Phthalaldehyde (OPA)-Mediated 2-Substituted Isoindole Core Formation and Applications", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 87, no. 5, 4 March 2022 (2022-03-04), pages 2551 - 2558, XP093142251, ISSN: 0022-3263, DOI: 10.1021/acs.joc.1c02496
LI BO, WANG LAN, CHEN XIANGXIANG, CHU XIN, TANG HONG, ZHANG JIE, HE GANG, LI LI, CHEN GONG: "Extendable stapling of unprotected peptides by crosslinking two amines with o-phthalaldehyde", NATURE COMMUNICATIONS, NATURE PUBLISHING GROUP, UK, vol. 13, no. 1, 14 January 2022 (2022-01-14), UK, pages 311, XP093142254, ISSN: 2041-1723, DOI: 10.1038/s41467-022-27985-7
Attorney, Agent or Firm:
CHINA TRUER IP (CN)
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