Simple exploration of 66491-03-0

66491-03-0 7-Amino-3,4-dihydroisoquinolin-1(2H)-one 13152844, aisoquinoline compound, is more and more widely used in various.

66491-03-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.66491-03-0,7-Amino-3,4-dihydroisoquinolin-1(2H)-one,as a common compound, the synthetic route is as follows.

A solution of 7-amino-3,4-dihydroisoquinolin-1(2H)-one (1.01 g, 6.23 mmol) and N-chlorosuccinimide (832 mg, 6.23 mmol) in N,N-dimethylformamide (10 mL) was and heated to 55 C. for 5 hours. The mixture was poured into water and extracted with ethyl acetate (3¡Á). The combined ethyl acetate layers were concentrated, and residual DMF was removed on high vacuum overnight. The resulting dark oil was purified on silica gel (Biotage SNAP, 50 g, gradient of 50-100% ethyl acetate in heptanes) to give 7-amino-8-chloro-3,4-dihydroisoquinolin-1(2H)-one (Cpd X, 0.539 g, 44%) as a white solid. 1H NMR (400 MHz, DMSO-d6) delta 7.87 (br. s., 1H), 6.96 (d, J=8.19 Hz, 1H), 6.87 (d, J=8.19 Hz, 1H), 5.32 (s, 2H), 3.20 (dt, J=3.79, 6.17 Hz, 2H), 2.69 (t, J=6.24 Hz, 2H); MS 197 [M+H]+.

66491-03-0 7-Amino-3,4-dihydroisoquinolin-1(2H)-one 13152844, aisoquinoline compound, is more and more widely used in various.

Reference£º
Patent; PFIZER INC.; Collins, Michael Raymond; Kania, Robert Steven; Kumpf, Robert Arnold; Kung, Pei-Pei; Richter, Daniel Tyler; Sutton, Scott Channing; Wythes, Martin James; US2015/361067; (2015); A1;,
Isoquinoline – Wikipedia
Isoquinoline | C9H7N – PubChem

 

Brief introduction of 66491-03-0

The synthetic route of 66491-03-0 has been constantly updated, and we look forward to future research findings.

66491-03-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.66491-03-0,7-Amino-3,4-dihydroisoquinolin-1(2H)-one,as a common compound, the synthetic route is as follows.

Intermediate 16 (400mg) was dissolved with 10ml of acetone, was added trimethylsilyl cyanide (2ml) and acetic acid 2ml, sealed tube, heated to 60 deg.] C overnight.The reaction was cooled to room temperature, concentrated under reduced pressure after adding water, an aqueous solution (100ml ¡Á 3) and extracted with ethyl acetate, the ethyl acetate layer was washed with water and saturated brine, dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give a yellow oil It was flash column chromatography (petroleum ether: ethyl acetate = 2: 1) to give the intermediate 17 (460mg).

The synthetic route of 66491-03-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences,; Duan, WenHu; Wan, huixin; Xia, GuangXin; Mei, deCheng; Lin, Yipeng; Liu, Xuejun; Shen, JingKang; (53 pag.)CN103804358; (2016); B;,
Isoquinoline – Wikipedia
Isoquinoline | C9H7N – PubChem