The synthetic method of compound sch-79797
A technology of SCH-79797 and SCH79797, which is applied in the field of drug synthesis and can solve problems such as complex conditions and long synthetic routes of compounds
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[0019] Embodiments of the present application provide a method for synthesizing a compound SCH79797, comprising the following steps:
[0020] S01: The first reaction was 1-(4-isopropylphenylmethyl)-1H-5-aminoindole and dimethyl cyanimine absurdate to give the intermediate shown in Formula I below;
[0021] S02: The intermediate shown in formula I was reacted with cyclopropanine for a second reaction to give compound SCH-79797;
[0022]
[0023] Embodiment of the present application provides a synthesis method of compound SCH-79797, only two steps of chemical reaction can be obtained, specifically, first 1- (4-isopropylphenylmethyl) -1H-5-aminoindole and cyanoimide dimethylate as raw material for reaction, to obtain the intermediate shown in formula I, and then the intermediate with cyclopropanine can be reacted to obtain compound SCH-79797; the synthesis method is completed by the above two-step reaction to complete the preparation of compound SCH-79797, It has the characteristi...
Embodiment 1
[0036] Preparation of intermediates shown in Formula I
[0037]
[0038]In a 500mL trineck bottle, acetonitrile 250mL, dimethyl cyanoimide 14.6 g (100mmol), 1-(4-isopropylphenylmethyl)-1H-5-aminoindole 26.4g (100mmol) were added sequentially, and the reaction was 20 hours at 160 °C. After the end of the reaction, 300ml of n-hexane was added to the system, the solids were precipitated, filtered, and dried to give 35.1g of class white solid products, that is, intermediate formula I, with a purity of 98% and a yield of 97%.
[0039] The structure of the product obtained by the above steps was confirmed by mass spectrometry and MRI, and the results were: 1 H NMR(400MHz,DMSO-d 6 )δ7.67(d,J＝9.0Hz,1H),7.41(d,J＝8.9Hz,1H),7.34(d,J＝3.0Hz,1H),7.21(m,2H),7.06(m,2H),6.75(d,1H,J＝3.0Hz),5.69(br,2H),5.43(s,2H),2.95-2.90(m,1H),2.48(s,3H),1.26(d,6H, J＝5.5Hz).MS(ESI):[M+H + ]363.50.
Embodiment 2
[0041] Preparation of intermediates shown in Formula I
[0042] In the 500mL trineck bottle, N, N-dimethylformamide 250mL, dimethyl cyanoimine wild acid dimethyl ester 14.6 g (100mmol), 1-(4-isopropylphenylmethyl)-1H-5-aminoindole 26.4g (100mmol) were added sequentially, and the reaction was 170 °C for 15 hours. After the end of the reaction, 300ml of n-hexane was added to the system, the solid was precipitated, filtered, and dried to obtain 34.5g of white solid products, that is, intermediate formula I, with a purity of 98% and a yield of 95%.
[0043] The product obtained by the above step is confirmed by mass spectrometry and NUCLEAR magnetic resonance and embodiment 1 is the same.
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