With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.
A mixture of intermediate 1 (2.42 g, 4.28 mmol)DMAP (1.05 g, 8.59 mmoL),EDCI (1.07 g, 5.58 mmoL) andDichloromethane (30.0 mL) was added to the reaction flask 1.A solution of 4- [4 – [[2- (4-chlorophenyl) -4,4-dimethyl-1-cyclohexen-1-yl] methyl] -1-piperazine] 1H-pyrrolo [2,3-b] pyridin-5-yloxy) benzoic acid (2.5 g, 4.4 mmoL)Triethylamine (0.87 g) andDichloromethane (12.0 mL) was added to the reaction flask 2. [The solution in the reaction flask 2 was slowly added dropwise to the reaction flask 1,After the dropwise addition was stirred overnight, the TLC monitored the reaction completely.N, N’-dimethylethylenediamine (0.94 g) was added,Oil bath to 55 ,Then add 10% acetic acid (18.5 mL) and stir overnight.Cooling, liquid separation. The organic phase was washed once with 10% acetic acid (18.5 mL).Dichloromethane (7.5 mL) was added to the organic phase.Followed by 5% aqueous sodium bicarbonate (18.5 mL) and5% sodium chloride (18.5 mL).The solvent was evaporated under reduced pressure and the residue was separated by flash column chromatography. The elution solvent was dichloromethane / methanol = 10/1,2.4 g of a white solid, yield 63%., 1235865-77-6
1235865-77-6 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid 66713100, apiperazines compound, is more and more widely used in various fields.
Reference：
Patent; Suzhou Guokuang Pharmaceutical Technology Co., Ltd.; Mei Desheng; Liu Aifeng; (50 pag.)CN106608895; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics