Synthetic Route of 153505-37-4, These common heterocyclic compound, 153505-37-4, name is 4-Bromo-5-fluorobenzene-1,2-diamine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
To a solution of 4-bromo-5-fluorobenzene-1,2-diamine (4.50 g, 21.95 mmol), (S)-2-((tert-butoxycarbonyl)amino)-3 ,3-dimethylbutanoic acid (5.08 g, 21.95 mmol), DIPEA (3.83 mL, 21.95 mmol) in CH2C12 (200 mL) at 0 C was added HATU (8.35 g, 21.95 mmol). The reaction mixture was stirred for 18 h at RT. After which, water (500 mL) was added into the reaction mixture and extracted with ethyl acetate (3 x100 mL). The organic layer was washed with brine, dried (Na2SO4) and concentrated to afford Bla and/or ite regioisomer (10.0 g) as brown liquid. Crude was taken fornext step without further purification. LC/MS: Anal. Calcd. for [M+Hj mz C17H26BrFN3O3: 420.11; found 420.1.
The synthetic route of 153505-37-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; FRENNESSON, David B.; HEWAWASAM, Piyasena; LOPEZ, Omar D.; NGUYEN, Van N.; SAULNIER, Mark G.; TU, Yong; WANG, Alan Xiangdong; WANG, Gan; XU, Ningning; NIMJE, Roshan Yadavrao; RAHAMAN, Hasibur; GUPTA, Samayamunthula Venkata Satya Arun Kumar; MEANWELL, Nicholas A.; BELEMA, Makonen; (107 pag.)WO2017/23631; (2017); A1;,
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