تفاعل #88760

ord-1406e6c5b41a4eb8a1f45c72c3a5c04b

المذيبات

ظروف التفاعل

درجة الحرارة
60°CELSIUS
الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    درجة الحرارةcooled to RT
  2. 2
    ترشيحfiltered
  3. 3
    تركيزThe filtrate was concentrated

الإجراء التجريبي

To a solution of 6-bromo-5-((4-chlorophenyl)(hydroxy)methyl)-1-methyl-3-(3-(tetrahydro-2H-pyran-2-yloxy)propyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione (800 mg, 1.50 mmol) in HCOOH (10 mL) was added Zn dust (484 mg, 7.50 mmol). The reaction was heated at 60° C. for 2 h, cooled to RT and filtered. The filtrate was concentrated to give 3-(6-bromo-5-(4-chlorobenzyl)-1-methyl-2,4-dioxo-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propyl formate (419 mg, 60% yield as a solid. LCMS: MH+ 466 and TR=1.589 min. Used without further purification.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US09440972B2uspto-grants-2016_09