5-Chloro-2-picolinic acid → 5-Chloro-pyridine-2-carboxylic acid [3-((R)-5-amino-3-methyl-1,1-dioxo-1,2,3,6-tetrahydro-1lambda6-[1,4]thiazin-3-yl)-4-fluoro-phenyl]-amide

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Reaction Steps

Prepared from 5-chloropicolinic acid (73.5 mg, 466 μmol, Eq: 1.1) and (R)-5-(5-amino-2-fluoro-phenyl)-5-methyl-1,1-dioxo-1,2,5,6-tetrahydro-1λ6-[1,4]thiazin-3-ylamine (115 mg, 424 μmol, Eq: 1.00) as described for example 2 (method b) to give the title compound (80 mg, 195 μmol, 45.9% yield) as a light yellow solid. MS (ISP): m/z=411.4 [(M+H)+] and 413.2 [(M+2+H)+].

Provenance & Evidence