3-环己基-1H-吲哚-6-甲酸作为医药中间体,用于相关药物的合成制备。
医药
合成路线 1(1. 合成:494799-17-6)
产率:90%
合成条件:With hydrogen In tetrahydrofuran; methanol for 14 h;
实验步骤:第2步; 甲基-3-环己基-1H-吲哚-6-羧酸酯; 将在THF / M eOH(0.5M,1:1,v / v)中的3-环己烯基-1H-吲哚-6-羧酸(来自步骤1)的溶液(0.5M)在Pd(OH)上氢化14小时。 )在60psi下2 / C(0.1当量,20%)。 通过硅藻土垫(TM)过滤除去催化剂。 将滤液蒸发至干,得到3-环己基-1H-吲哚-6-羧酸(90%),为白色固体1H NMR(300MHz,DMSO-d6,300K)6 1.20-1.53(m,SH) ,L70-L87(m,3H),1.90-2.02(m,2H),2.69-2.86(m,1H),7.40(s,1H),7.55-7.65(rn,2H),8.0(s,1H) ,11.40(s,1H); MS(ES + m / z 244(M + H)+。将上述化合物的MeOH(0.4M)溶液在0℃下用亚硫酰氯(0.5当量)处理并回流24小时。 在真空下除去挥发物,得到标题化合物(100%),为固体。
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