Reacción #11062

Ecuación de reacción

1j

(S)-[(4-{[(3-amino-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carbonyl)-amino]-methyl}-phenyl)-imino-methyl]-carbamic acid tert-butyl ester

methanesulfonyl chloride

→

intermediate 16a

Rendimiento 22.0%

(S)-[imino-(4-{[(3-methanesulfonylamino-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carbonyl)-amino]-methyl)-phenyl)-methyl]-carbamic acid tert-butyl ester

Rendimiento 22.0%

Disolventes

EtOAc

pyridine

Condiciones de reacción

Tratamiento posterior

1. 1
   Lavadowashed with H2O (2×) and brine
2. 2
   Secadodried (Na2SO4)
3. 3
   Concentraciónconcentrated

Procedimiento

To a solution of 1j (50 mg, 0.117 mmol) in 0.5 mL pyridine at 0° C. was added methanesulfonyl chloride (14.8 mg, 0.129 mmol). The solution was stirred at rt for 16 h. The mixture was diluted with 50 mL EtOAc, washed with H2O (2×) and brine, dried (Na2SO4) and concentrated to afford 13 mg (22%) of intermediate 16a. MS (ESI) 505.0 (M+H+).

Fuente