With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.27810-64-6,Isoquinoline-5-carboxylic acid,as a common compound, the synthetic route is as follows.
General procedure: To a stirring solution of corresponding picolinic or nicotinic acids (1.0 eq.), EDCI (1.5 eq.) and HOBt (1.0 eq.)in CH2Cl2 at room temperature was added Et3N (2 eq.) dropwise, followed by the amine. The resultedmixture was stirred for 16 h and afterwards diluted by excess amount of CH2Cl2. The organic solution waswashed by water and dried over Na2SO4. A yellow residue was obtained after concentration and purified byflash column on silica gel to afford compound S2. To a solution of S2 (1.0 eq.) in THF at 78 was addedn-BuLi (1.1 eq.) or LDA (1.1 eq.) dropwise. The resulted mixture was stirred at this temperature for 15 min.A solution of corresponding acryloyl chloride (1.3 eq. while using n-BuLi and 2.5 eq. while using LDA) wasadded dropwise at 78. The reaction was warmed to room temperature gradually and stirred for another5 h . Afterwards, the reaction mixture was diluted with EtOAc and the organic solution was washed bywater and dried over Na2SO4. A brown residue was obtained after concentration and purified by flashcolumn on silica gel to afford the compound 4. Analytical data of 4q and 4r are consistent with the previousreports
27810-64-6, 27810-64-6 Isoquinoline-5-carboxylic acid 260936, aisoquinoline compound, is more and more widely used in various fields.
Reference£º
Article; Ma, Jiajia; Strieth-Kalthoff, Felix; Dalton, Toryn; Freitag, Matthias; Schwarz, J. Luca; Bergander, Klaus; Daniliuc, Constantin; Glorius, Frank; Chem; vol. 5; 11; (2019); p. 2854 – 2864;,
Isoquinoline – Wikipedia
Isoquinoline | C9H7N – PubChem