تفاعل #6976

ord-4666dd45d7d6434b83112ed5ee7716cf

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىThe above reaction mixture
  2. 2
    غسيلwashed with 10% NaHCO3 (3×5 mL), and 10% LiCl (5 mL)
  3. 3
    تجفيفThe organic layer was dried over Na2SO4
  4. 4
    تركيزconcentrated
  5. 5
    أخرىthe residue was purified by preparative HPLC

الإجراء التجريبي

To a solution of 4-fluoro-3-{[2-(pyridin-2-ylamino)-thiazol-5-ylmethyl]-amino}-benzoic acid (35 mg, 0.10 mmol) in DMF (1 mL) at RT, cyclopropylmethyl amine (14 mg 0.20 mmol) was added followed by the addition of BOP reagent (53 mg, 0.12 mmol). The above reaction mixture was stirred for 2 h, diluted with EtOAc (10 mL), washed with 10% NaHCO3 (3×5 mL), and 10% LiCl (5 mL). The organic layer was dried over Na2SO4, concentrated and the residue was purified by preparative HPLC to give the title compound as a off-white solid (33 mg, 83%). (M+H)+=398.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07084160B2uspto-grants-2006_08