Azoalkene chemistry provides practical access to 5-aminopyrazoles selectively protected at the N-1 position Научная публикация
| Журнал |
Tetrahedron Letters
ISSN: 0040-4039 , E-ISSN: 1873-3581 |
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| Вых. Данные | Год: 2026, Том: 178, Номер статьи : 155987, Страниц : DOI: 10.1016/j.tetlet.2026.155987 | ||
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Реферат:
5-Aminopyrazoles are extensively used as building blocks in medicinal chemistry. However, selective protection of endo- and exocyclic nitrogen atoms is challenging. Here, we describe a convenient protocol for the synthesis of 1-Boc-protected 5-aminopyrazoles through Michael addition of cyanide to azoalkenes followed by spontaneous cyclization of the resulting α-cyanohydrazones. The process utilizes readily available α-halohydrazones, acetone cyanohydrin as a safer substitute for cyanide, and aqueous DMSO as the reaction medium. The method enables further synthetic diversification of the resulting 1-Boc-5-aminopyrazoles through reactions with electrophilic agents.
Библиографическая ссылка:
Kokuev A.O.
, Sukhorukov A.Y.
Azoalkene chemistry provides practical access to 5-aminopyrazoles selectively protected at the N-1 position
Tetrahedron Letters. 2026. V.178. 155987 . DOI: 10.1016/j.tetlet.2026.155987 WOS Scopus OpenAlex
Azoalkene chemistry provides practical access to 5-aminopyrazoles selectively protected at the N-1 position
Tetrahedron Letters. 2026. V.178. 155987 . DOI: 10.1016/j.tetlet.2026.155987 WOS Scopus OpenAlex
Даты:
| Поступила в редакцию: | 5 дек. 2025 г. |
| Опубликована online: | 6 февр. 2026 г. |
Идентификаторы БД:
| Web of science: | WOS:001686950400001 |
| Scopus: | 2-s2.0-105029418407 |
| OpenAlex: | W7126379577 |
Цитирование в БД:
| БД | Цитирований |
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| OpenAlex | Нет цитирований |
| Scopus | Нет цитирований |