Rh-catalyzed C-H functionalization of the (Pyrazol-5-yl)pyridine core of GBT-440
| Title | Rh-catalyzed C-H functionalization of the (Pyrazol-5-yl)pyridine core of GBT-440 |
| Publication Type | Journal Article |
| Year of Publication | 2023 |
| Authors | Kalshetti, RG, Halnor, SV, Ramana, CV |
| Journal | Synthesis-Stuttgart |
| Volume | 55 |
| Issue | 21 |
| Pagination | 3600-3609 |
| Date Published | NOV |
| Type of Article | Article |
| ISSN | 0039-7881 |
| Keywords | C-H activation, cross dehydrogenative coupling, diazo ester, GBT-440, Rh catalysis, TIPS-EBX |
| Abstract | The Rh-catalyzed cross dehydrogenative coupling (CDC)/alkylation of the pyrazolylpyridine unit of GBT-440 proceeded smoothly under ambient conditions and selectively on the pyrazole unit while directed by the pyridine. The scope of these reactions was established by employing simple as well as conjugated olefins for CDC and various diazo esters and the TIPS-EBX reagent for alkylation. At the outset, a focused small molecule library around the bis-heterocyclic core of GBT440 was developed via C-H functionalization. |
| DOI | 10.1055/a-2116-6734 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 2.6 |
Divison category:
Organic Chemistry
Database:
Web of Science (WoS)
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