Organocatalytic and Scalable Syntheses of Unsymmetrical 1,2,4,5‐Tetrazines by Thiol‐Containing Promotors

• Published in: Angewandte Chemie International Edition Vol. 58; no. 4; pp. 1106 - 1109
• Main Authors: Mao, Wuyu, Shi, Wei, Li, Jie, Su, Dunyan, Wang, Xiaomeng, Zhang, Lyuye, Pan, Lili, Wu, Xiaoai, Wu, Haoxing
• Format: Journal Article
• Language: English
• Published: WEINHEIM Wiley 21.01.2019; Wiley Subscription Services, Inc
• Edition: International ed. in English
• Subjects: annulations; Catalysts; Chemistry; Chemistry, Multidisciplinary; Functional groups; heterocycles; Hydrazine; Hydrazines; Nitriles; Organic chemistry; organocatalysis; Peptides; Physical Sciences; Science & Technology; synthetic methods; DRUG; ARYLTETRAZINES; ONE-POT SYNTHESIS; RELEASE; MOLECULES; PROBES; organocatalysis; TETRAZINE DERIVATIVES; nitriles; annulations; heterocycles; CHEMISTRY; CLICK; synthetic methods

Despite the growing application of tetrazine bioorthogonal chemistry, it is still challenging to access tetrazines conveniently from easily available materials. Described here is the de novo formation of tetrazine from nitriles and hydrazine hydrate using a broad array of thiol‐containing catalysts,...