Hydrochloric Acid → (R)-1-methyl-10-(3-methyl-azetidin-3-yl)-3,5-dihydro-10H-6-oxa-3,4,10,11b-tetraaza-cyclopenta[b]phenanthren-2-one hydrochloride

Participants

Reaction Steps

To a solution of HCl (4M in EtOAc, 160 mL) was added 3-[(R)-7-((E)-2-ethoxy-vinyl)-4-methyl-3-oxo-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-ylamino]-3-methyl-azetidine-1-carboxylic acid tert-butyl ester (16 g, 33.9 mmol) at 0° C. and the reaction mixture was stirred for 30 min. The reaction mixture was concentrated in vacuo to give crude (R)-1-methyl-10-(3-methyl-azetidin-3-yl)-3,5-dihydro-10H-6-oxa-3,4,10,11b-tetraaza-cyclopenta[b]phenanthren-2-one hydrochloride (10 g, 91%), which was used in the next step without further purification. LC/MS (Table 1, Method 25) Rt=0.627 min; MS m/z: 326 [M+H]+

Provenance & Evidence