Tacrolimus-13C,D2 → HCID 57266865、化合物

関与物質

反応手順

To a stirred solution of 17-allyl- 1,14-dihydroxy-12-[2'-(4"-hydroxy-3"-methoxycyclohexyl)1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9 ]octacos-18-ene-2,3,10,16-tetraone (300 mg, 0.374 mmol) in 9 ml MeOH was added dropwise at RT a solution of NaBH4 (0.12 mmol) in 2 ml isopropanol. After stirring at RT for 15 minutes the reaction was quenched by pouring into 1.5 ml acetic acid in ice and the mixture was extracted with ethyl acetate (3×50 ml). The combined organic layers were washed with sat. NaHCO3 (1×50 ml) and water (1×50 ml) and dried over MgSO4. Evaporation of solvent gave 320 mg of crude product which was purified by prep TLC (10% i-PrOH/CH2Cl2) to give 127 mg (42% yield) of the title compound (with NMR and mass spectra consistent with the structure).

情報源と証拠