Simple exploration of 1-(3,3-Diphenyl-N-methylpropylamino)-2-methyl-2-propanol

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,100442-33-9, its application will become more common.

Reference of 100442-33-9, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 100442-33-9 as follows.

Example 1: Preparation of crude l,4-dihvdro-2,6-dimethyl-4-(3- nitrophenyl)-3 ,5 -pyridinedicarboxylic acid [2-|Y3,3- diphenylpropyl)methylamino~|- 1,1 -dimethyl ethyl] methyl ester hydrochloride (crude lercanidipine hydrochloride)2.31 mL of triethylamine and 2.4 mL of diethylchlorophosphate were added to 5.0 g of 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-l,4- dihydropyridine-3-carboxylic acid (2) in 50 mL of toluene. The mixture was stirred at room temperature for one hour. After formation of a substituted phosphonoester derivative (5) as an intermediate was confirmed by thin layer chromatography (TLC), 4.49 g of 2, N-dimethyl-N-(3,3-diphenylpropyl)-l-amino-2-propanol (3) was added thereto (5). The resulting mixture was refluxed for 4 hours. The reaction mixture was treated with activated carbon and was then concentrated under reduced pressure to remove toluene therefrom. The residue was dissolved in 30 mL of ethyl acetate. The organic phase was washed sequentially with 11 mL of a 10% NaOH aqueous solution, 11 mL of distilled water, 13.1 mL of 6N HCl and 11 mL of distilled water. An organic layer was separated, dried with activated carbon and anhydrous sodium sulfate for 30 min and concentrated under reduced pressure. The residue was dissolved in 15.7 mL of tetrahydrofuran and was then seeded with 50 mL of lercanidipine hydrochloride. The lercanidipine hydrochloride (dispersion) was stirred at 20 to 25 C for 24 hours, filtered and dried under vacuum to obtain 8.3 g of crude lercanidipine hydrochloride (theoretical yield: 85.1%).IH NMR (DMSO-d, 400MHz) (ppm): 10. 8 -9.4 (bb, IH), 9.5 (bs, IH), 8.30 – 8.05 (m, 2H), 7.85 -7.60 (m, 2H), 7.55 -7.20 (m, 10H), 5.05 (s, IH), 4.15 – 3.35 (m, 6H), 3.20 -2.15 (m, 13H), 2.6 (s, 3H), 1.50 (s, 6H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,100442-33-9, its application will become more common.

Reference:
Patent; DONGWOO SYNTECH CO., LTD; WO2008/82041; (2008); A1;,
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