A new synthetic route of 135484-83-2

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Methyl 2-amino-4-bromobenzoate, and friends who are interested can also refer to it.

Synthetic Route of 135484-83-2, 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. 135484-83-2 name is Methyl 2-amino-4-bromobenzoate, This 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.

Example 16a4-Bromo-2-(2,5-dichloro-pyrimidin-4-ylamino)-benzoic acid methyl ester2-Amino-4-bromo-benzoic acid methyl ester (1.2g, 5.0 mmol) was combined with2,4,5-trichloro-pyrimidine (5.33 mL, 46.5 mmol) and EtN(i-Pr)2 (0.95 mL, 5.5 mmol), and the mixture was warmed to 120C. After 16 hours the excess 2,4,5-trichloro-pyrimidine was removed under high vacuum, and the residue was then treated with 1 : 1 MeOH: water. The resulting solid was filtered, retriturated with 1 : 1 MeOH: water, re filtered, and the resulting solid triturated in MeOH at 50C. After filtering, the solid was rinsed liberally with MeOH. After air drying 4-Bromo-2-(2,5-dichloro-pyrimidin-4-ylamino)-benzoic acid methyl ester was recovered in 52% yield as a brown solid and was carried on for subsequent steps without further manipulation. LC/MS: M+H= 377.9.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Methyl 2-amino-4-bromobenzoate, and friends who are interested can also refer to it.

Reference:
Patent; CEPHALON, INC.; BRESLIN, Henry J.; DORSEY, Bruce; OTT, Gregory R.; WO2012/125603; (2012); A1;,
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