- Molybdenum-silver co-catalyzed cycloaddition of alkynes with: N -isocyanoiminotriphenylphosphorane (NIITP): An efficient strategy for the synthesis of monosubstituted pyrazoles
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A new molybdenum-silver co-catalyzed [3+2] cycloaddition of alkynes with N-isocyanoiminotriphenylphosphorane (NIITP) has been described. The NIITP serves as a non-toxic, facile "CNN" source. Over 30 substrates were successfully converted to the desired compounds in good to excellent yields.
- Mi, Pengbing,Lang, Jiajia,Lin, Shaojian
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supporting information
p. 7986 - 7989
(2019/07/10)
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- Silver-Mediated [3 + 2] Cycloaddition of Alkynes and N-Isocyanoiminotriphenylphosphorane: Access to Monosubstituted Pyrazoles
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A silver-mediated [3 + 2] cycloaddition of "CNN" and "C≡C" for constructing pyrazoles has been described. The "CNN" building block used is N-isocyanoiminotriphenylphosphorane, which is a stable, safe, easy-to-handle, and odorless solid isocyanide. The reaction is characterized by its mild conditions, broad substrate scope, and excellent functional group tolerance.
- Yi, Fanhua,Zhao, Wanjun,Wang, Zikun,Bi, Xihe
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supporting information
p. 3158 - 3161
(2019/05/10)
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- Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus
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The discovery and initial optimization of a series of phenylalanine based agonists for GPR142 is described. The structure-activity-relationship around the major areas of the molecule was explored to give agonists 90 times more potent than the initial HTS hit in a human GPR142 inositol phosphate accumulation assay. Removal of CYP inhibition by exploration of the pyridine A-ring is also described.
- Lizarzaburu, Mike,Turcotte, Simon,Du, Xiaohui,Duquette, Jason,Fu, Angela,Houze, Jonathan,Li, Leping,Liu, Jinqian,Reagan, Jeff,Yu, Ming,Medina, Julio C.,Murakoshi, Michiko,Oda, Kozo,Okuyama, Ryo,Nara, Futoshi
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p. 5942 - 5947,6
(2020/07/30)
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- PHENYLALANINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS
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Provided herein are compounds of formula I: wherein A, B, X, R1 , R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions
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Page/Page column 58
(2010/09/03)
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- SUBSTITUTED HETEROCYCLYL-PHENYLFORMAMIDINES AND SALTS THEREOF
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Compounds of the formula STR1 wherein R is hydrogen or methyl;R 1 is straight or branched alkyl of 1 to 6 carbon atoms, hydroxy(alkyl of 1 to 6 carbon atoms), mono-or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 cabon atoms) thio(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R 2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andX is pyrazol-3-yl, 1,2,4-triazol-3-yl, pyridin-2-yl, pyridin-3-yl, thiazol-4-yl, 2-methyl-thiazol-4-yl or 2-methylamino-thiazol-4-yl;tautomers thereof, and non-toxic, pharmacologiically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics and gastric acid secretion inhibitors.
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