With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.23190-16-1,(1R,2S)-2-Amino-1,2-diphenylethanol,as a common compound, the synthetic route is as follows.
To a 5 L round bottom flask equipped with an overhead stirrer, thermocouple and distillation head, was charged 550 g (2.579 mol) of (1 R,2S)- diphenyl-2-aminoethanol, 457 g (3.868 mol, 1.5eq) of diethylcarbonate, 18 g (0.258 mol, 0.1 eq) of NaOEt in 100 mL of EtOH and 3.5 L of toluene. The reaction was heated until an internal temperature of 90C was reached and EtOH distillation began. The reaction was refluxed until an internal temperature of 110C was reached (7 hours). For every 500 mL of solvent that was removed via the distillation head, 500 mL of toluene was added back to the reaction. A total of about 1.6 L of solvent was removed. The reaction was allowed to cool to room temperature and then filtered on a 3 L coarse fritted funnel with 2 psig N2. Nitrogen was blown over the cake overnight (at)o give 580 g (94% yield) of the titled nom””””” ””d” 9,-..C.U.(at), l:(at)VQ”; ‘I <"Q'.(at)(at) Up(at),.,; ',r1" (at)'(at) (at) (at).(at).(at) (at)-77 1'Cf'; 41i), ..(at)(at) ^(at)''1 I or(at)r(at)1 (at),f3rr:.(at)i ....u..(at) " ' (at).V.(at)_7(at)dli (at) ",-JVV Jc;;;J7Jv (at)L.-, U- -(at)t 'H'o(at)(at)-:J """.v (at)' "(at)(at) fUSD5 -/: q,78V;",j (at)(at)-j -(at), t(at).3J(at):, (at):_/(at).:::: , OJ (at), :=: ?Q(at)':::'::' 23190-16-1, As the paragraph descriping shows that 23190-16-1 is playing an increasingly important role.
Reference£º
Patent; PFIZER PRODUCTS INC.; WO2005/102389; (2005); A2;,
Chiral Catalysts
Chiral catalysts – SlideShare