With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.19752-84-2,Tetrahydro-2H-pyran-3-ol,as a common compound, the synthetic route is as follows.
EXAMPLE IDSTEP 2: Displacement of the leaving group with 6 membered 3- hydroxyheteroalkoxyalkyl compounds for the synthesis of 42-0-(heteroaIkoxyaIkyl) rapamycin compound.Preparation of 42-0-(tetrahydropyran-3-yl), rapamycin (Merilimus 3)A reaction flask containing triflate intermediate of step-1 was further cooled to -50 C temperature and 6.07 grams (46mmol) of N,N-di-n-butylethylamine (DNBEA) followed by 1.17 grams (13.8mmol) of tetrahydropyran-3-ol compound in methylene chloride were added. The reaction mixture was stirred at -10 C temperature for 12 hours. The reaction mixture was then allowed to warm to 15 C temperature and continuously stirred for 48 hours.The reaction mixture was further concentrated by evaporation under reduced pressure to provide a pale yellow viscous mass. The quantitative HPLC of reaction mass shows theoretical yield of 62%. This mass was purified by preparative HPLC (MeOH (65%): ACN (15%): H20 (20%)) to obtain the desired product in about 65% purity. Further purification was done by combiflash (0-40% EtOAc in Hexane) to get 42-0- (tetrahydropyran-3-yl) rapamycin compound having 97.3% purity by HPLC. Then stabilizing agent BHT in acetone was homogeneously mixed with purified compound and isolation & drying steps were carried out to get white solid powder of 42-0- (tetrahydropyran-3-yl) rapamycin compound. C56H87N014 Mol. Wt.: 998.2742-0-(tetrahydropyran-3-yl), rapamycin REACTION SCHEME-DThe 42-0-(tetrahydropyran-3-yl) rapamycin compound thus obtained was analytically identified., 19752-84-2
Big data shows that 19752-84-2 is playing an increasingly important role.
Reference£º
Patent; MERIL LIFE SCIENCES PVT. LTD; RANE, Dhananjay, Sharad; VYAS, Rajnikant, Gandalal; MINOCHA, Pramod, Kumar; WO2012/17449; (2012); A1;,
Tetrahydropyran – Wikipedia
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