With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1805-65-8,2-(tert-Butyl)-1H-indole,as a common compound, the synthetic route is as follows.
General procedure: In order to verify the feasibility of the reaction, azobenzene derivative 1a and 2-t-butyl-indole 2a as reactants and 10 mol% of phosphoric acid CP1 as a catalyst were reacted in DCM at room temperature as shown in the following formula. The reaction proceeded smoothly to give the shaft chiral arylindole 3a with a yield of 76% and an ee value of 87%. It can be seen that it is feasible to asymmetrically construct the axial chiral arylindole via an indole nucleophilic attack on azobenzene derivatives. Next, the catalysts with different chiral skeletons and substituents are screened. The aromatic ring skeleton and 3,3′-substituent of the catalyst have important influence on enantioselectivity. Among them, catalyst CP4 had the best results in terms of enantioselectivity (92% ee) and yield (99%).Reaction conditions: React with 1 a (0.10 mmol, 1.0 equiv.), 2a (0.12 mmol, 1.2 equiv.) And CP (10 mol%) in dichloromethane (2.0 mL) at room temperature.Further conditions were screened as shown in Table 1 to obtain optimal reaction conditions: 2a (1.1 eq.) Was added to 1a (1.0 eq.), 2.5 mol% CP4, 2.0 mL toluene solution and reacted at room temperature with 97% ee, 95% isolated yield gave the shaft chiral arylindole 3a.
1805-65-8, As the paragraph descriping shows that 1805-65-8 is playing an increasingly important role.
Reference£º
Patent; South University of Science and Technology of China; Tan Bin; Qi Liangwen; Mao Jianhui; (23 pag.)CN107501160; (2017); A;,
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