83164-33-4Relevant articles and documents
Ir-Catalyzed Ligand-Free Directed C-H Borylation of Arenes and Pharmaceuticals: Detailed Mechanistic Understanding
Mahamudul Hassan, Mirja Md,Mondal, Biplab,Singh, Sukriti,Haldar, Chabush,Chaturvedi, Jagriti,Bisht, Ranjana,Sunoj, Raghavan B.,Chattopadhyay, Buddhadeb
, p. 4360 - 4375 (2022/03/16)
An efficient method for Ir-catalyzed ligand free ortho borylation of arenes (such as, 2-phenoxypyridines, 2-anilinopyridines, benzylamines, benzylpiperazines, benzylmorpholines, benzylpyrrolidine, benzylpiperidines, benzylazepanes, α-amino acid derivatives, aminophenylethane derivatives, and other important scaffolds) and pharmaceuticals has been developed. The reaction underwent via an interesting mechanistic pathway, as revealed by the detailed mechanistic investigations by using kinetic isotope studies and DFT calculations. The catalytic cycle is found to involve the intermediacy of an Ir-boryl complex where the substrate C-H activation is the turnover determining step, intriguingly without any appreciable primary KIE. The method displays a broad range of substrate scope and functional group tolerance. Numerous late-stage borylation of various important molecules and drugs were achieved using this developed strategy. The borylated compounds were further converted into more valuable functionalities. Moreover, utilizing the benefit of the B-N intramolecular interaction of the mono borylated compounds, an operationally simple method has been developed for the selective diborylation of 2-phenoxypyridines and numerous functionalized arenes. Furthermore, the synthetic utility has been showcased with the removal of the pyridyl directing group from the borylated product to achieve ortho borylated phenol along with the ipso-borylation for the preparation of 1,2-diborylated benzene.
Process for the preparation of arylamides of heteroaromatic carboxylic acids
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Page/Page column 7, (2010/01/31)
A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each Anis nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1to R5being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6is hydrogen or C1-4-alkyl; and R7is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.
Solid mixtures based on sulfonylureas and adjuvants
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, (2008/06/13)
A solid ixture comprising a) an active ingredient from the group of the sulfonylureas and b) an alkyl ether of a copolymer of C2-C4-alkylene oxides.