As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 1196152-34-7, name is 2-Bromo-6-methoxypyridin-4-amine, molecular formula is C6H7BrN2O, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. COA of Formula: C6H7BrN2O
[00210] To a stirred solution of triphosgene (1 eq, 0.83 mmol) in DCM (16 ml_) at -20 C and under an atmosphere of N2 was added a solution of 2-bromo-6-methoxy-pyridin-4- ylamine (1 eq, 0.83 mmol) in DCM (6 ml_) followed by triethylamine (2.5 eq, 2.08 mmol). The reaction was stirred at -20 C for 15 mins then allowed to warm to RT and stirred at RT for 30 mins. The reaction was cooled to -20 C and a solution of ((1S,3R)-(3-amino-cyclopentyl)- carbamic acid benzyl ester in dry DCM (3 ml_) was added and the reaction stirred at -20 C for 15 mins then at RT for 90mins. More triethylamine (2 eq, 1.66 mmol) was added and the reaction was at RT for 1 h. The reaction was quenched with methanol and concentrated in vacuo. The crude was purified by column chromatography to benzyl N-[(1S,3R)-3-[(2-bromo- 6-methoxy-4-pyridyl)carbamoylamino]cyclopentyl]carbamate (311 mg, 81 %) as a light yellow gum. AnalpH2_MeOH_4min, Rt: 3.21 min; m/z 463/465[M+H]+
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Reference:
Patent; OXFORD UNIVERSITY INNOVATION LIMITED; RABBITTS, Terrence; QUEVEDO, Camilo; CRUZ, Abimael; PHILIPS, Simon; FALLON, Philip Spencer; DUNN, Jonathan Neil; FREEM, Joshua Robert; LEE, Lydia Yuen-Wah; TRAORE, Tenin; WILLIAMS, Sophie Caroline; (219 pag.)WO2019/145718; (2019); A1;,
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