تفاعل #794572

معادلة التفاعل

cis-3-(((benzyloxy)carbonyl)amino)cyclobutyl 4-methylbenzenesulfonate

2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one

potassium carbonate

→

benzyl (trans-3-(3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl)cyclobutyl)carbamate

المذيبات

DMF

DCM

ظروف التفاعل

المعالجة

1. 1
   أخرىReaction mixture
2. 2
   درجة الحرارةwas heated to 85° C. for 3 hr
3. 3
   أخرىat 110° C.
4. 4
   أخرىovernight
5. 5
   أخرىReaction mixture
6. 6
   غسيلwashed with water and brine
7. 7
   أخرىPurification by Biotage (0-10% MeOH/DCM)
8. 8
   أخرىproduced product

الإجراء التجريبي

To a solution of cis-3-(((benzyloxy)carbonyl)amino)cyclobutyl 4-methylbenzenesulfonate (0.563 g, 1.5 mmol) in DMF (3.00 ml) was added 2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one (FSSI, 0.225 g, 1.500 mmol) and potassium carbonate (EMD, 0.415 g, 3.00 mmol). The resulting mixture was heated to 50° C. overnight. Reaction mixture was heated to 85° C. for 3 hr then at 110° C. overnight. Reaction mixture was diluted with DCM and washed with water and brine. Purification by Biotage (0-10% MeOH/DCM) produced product. Material was advanced to the next step. M+1: 353.9

المصدر