Electric Literature of 327056-73-5, These common heterocyclic compound, 327056-73-5, name is 3-Chloro-5-fluorobenzonitrile, 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.
Step A. JV-(4- {(Iff): 1 :[(R)-[3-(Aminocarbonyl)-5-chlorophenoxy](4-chlorophenyl)methyl]” 4,414-trifluorobutyUbenzoyl)-beta-alanineSodium tert-butoxide (92 mg, 0.96 mmol) was added to a solution of 3-chloro-5- fluorobenzomtrile (67.9 mg, 0.359 mmol) and N-(4-{(1R)-l-[(R)~(4- chlorophenyl)(hydroxy)methyl]-4s4,4-trifluorobulyl}benzoyl)-beta-alanine (prepared using the procedures from INTERMEDIATE 1 and the saponification step of EXAMPLE I, 100 mg, 0.239 mmol) in DMF (3 mL), then the resulting brown mixture was stirred at 80 0C for 16 hours. The mixture was diluted with EtOAc, then washed with 2 N HCl (aq), then washed twice with water. The organic layer was then concentrated, and the resulting yellow residue was purified by reverse phase HPLC eluting with 30-100% MeCN/water + 0.1% TFA. Following lyophilization, this afforded the title compound. LC3 3.35 min. (M+H)+ 577.
The synthetic route of 327056-73-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERCK SHARP &; DOHME CORP.; KATS-KAGAN, Roman; STEVENSON, Christian, P.; LIAO, Xibin; FU, Qinghong; PARMEE , Emma, R.; LIN, Songnian; WO2010/98948; (2010); A1;,
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts