1286715-41-0Relevant academic research and scientific papers
COMPOUNDS AS CASEIN KINASE INHIBITORS
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Paragraph 00324-00325; 00328-00329, (2021/10/02)
Provided are novel casein kinase inhibitors, or pharmaceutically acceptable salts thereof. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also provided.
METHODS FOR INHIBITING CASEIN KINASES
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Paragraph 00205; 00206; 00209; 00210, (2021/10/02)
The present disclosure provides methods for inhibiting CK1 delta or CK1 epsilon activity, comprising administering an effective amount of the compound of Formula (I) to (IV), or a pharmaceutically acceptable salt thereof.
Transition metal-free cyclization of N-boc-N-propargylenamines
Chikayuki, Yuya,Higashiyama, Kimio,Ishikawa, Haruka,Kouno, Yasuaki,Sasaki, Shigeru,Teramoto, Hiroyoshi,Waki, Yoko,Yamauchi, Takayasu,Yonekawa, Shiori
, p. 719 - 746 (2020/07/13)
An efficient method for the synthesis of multi-substituted pyrroles was developed using basic cyclization of readily accessible N-Boc-N-propargylenamines. Despite the basic conditions, cleavage of the N-Boc group occurred easily. The process was rapid and afforded N-H-pyrroles with wide functional group tolerance in high yields.
Regioselective synthesis of 2,3,4- or 2,3,5-trisubstituted pyrroles via [3,3] or [1,3] rearrangements of O-vinyl oximes
Wang, Heng-Yen,Mueller, Daniel S.,Sachwani, Rachna M.,Kapadia, Rachel,Londino, Hannah N.,Anderson, Laura L.
, p. 3203 - 3221 (2011/06/24)
The regioselective synthesis of 2,3,4- or 2,3,5-trisubstituted pyrroles has been achieved via [3,3] and [1,3] sigmatropic rearrangements of O-vinyl oximes, respectively. Iridium-catalyzed isomerization of easily prepared O-allyl oximes enables rapid access to O-vinyl oximes. The regioselectivity of pyrrole formation can be controlled by either the identity of the α-substituent or through the addition of an amine base. When enolization is favored, a [3,3] rearrangement followed by a Paal-Knorr cyclization provides a 2,3,4-trisubstituted pyrrole; when enolization is disfavored, a [1,3] rearrangement occurs prior to enolization to produce a 2,3,5-trisubstituted pyrrole after cyclization. Optimization and scope of the O-allyl oxime isomerization and subsequent pyrrole formation are discussed and mechanistic pathways are proposed. Conditions are provided for selecting either the [3,3] rearrangement or the [1,3] rearrangement product with β-ester O-allyl oxime substrates.
