1260878-78-1Relevant articles and documents
HETEROARYL PLASMA KALLIKREIN INHIBITORS
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Paragraph 0183; 0200, (2021/03/19)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
PLASMA KALLIKREIN INHIBITORS AND USES THEREOF
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Paragraph 0605; 0606, (2021/03/19)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Regioselective amidomethylation of 4-chloro-3-fluoropyridine by metalation and minisci-type reactions
Papaioannou, Nikolaos,Fray, M. Jonathan,Rennhack, Andreas,Sanderson, Thomas J.,Stokes, Jamie E.
, p. 12067 - 12079 (2020/11/10)
The synthesis of a series of 2-amidomethylated pyridines (3-8) was investigated, starting from 4-chloro-3- fluoropyridine. Kinetic deprotonation at -75 °C followed by reaction with DMF gave 2-formyl-4-chloro-3-fluoropyridine 10 regioselectively, which was converted to 2-aminomethyl analogue 1 via sulfinamide 2. Alternatively, Minisci-type amidomethylation under Ag+/persulfate or photoredox-mediated conditions using a series of amino acid derivatives gave (3-8, 19, and 34) in 30-74% yield and isomer ratios in the range 6.7:1 to >50:1. The latter methods gave overall yields similar to that of the deprotonation approach, but were shorter and more amenable to scale-up. In particular, N-Boc analogue 8 was obtained in a single step. The amidomethylations of another six 3-fluoropyridines under the photoredox conditions were briefly examined.
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
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, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.