Extracurricular laboratory: Synthetic route of C16H17NO6

Adding a certain compound to certain chemical reactions, such as: 88150-75-8, name is Ethyl 4-(2-(1,3-dioxoisoindolin-2-yl)ethoxy)-3-oxobutanoate, belongs to indolines-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 88150-75-8, Formula: C16H17NO6

Adding a certain compound to certain chemical reactions, such as: 88150-75-8, name is Ethyl 4-(2-(1,3-dioxoisoindolin-2-yl)ethoxy)-3-oxobutanoate, belongs to indolines-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 88150-75-8, Formula: C16H17NO6

To a solution of ethyl 4-(2-phthalimidoethoxy)acetoacetate in toluene was added 3000 ml of isopropyl alcohol, 564 g of 2-chlorobenzaldehyde was added with stirring, 17 5g acetic acid, 24.8g piperidine; 20 ~ 30 C, stirring 9 ~ 10h, adding 589g beta-aminocrotonic acid methyl ester, heating to 55 ~ 58 C, and stirring at 55 ~ 58 C reaction, stirring 7h sampling, TLC plate to confirm the end of the reaction, cooling to below 25 C, adding 3200ml acetic acid; then seeded to 0 ~ 5 C, the same temperature for 5h, crystallization; filtration crystallization, with 800ml isopropyl alcohol washing, the wash was run twice (400 ml each) and dried under reduced pressure to give 1611 g of phthaloyl amlodipine in a yield of 76.1%.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Ethyl 4-(2-(1,3-dioxoisoindolin-2-yl)ethoxy)-3-oxobutanoate, and friends who are interested can also refer to it.

Reference:
Patent; Qianhui Pharmaceutical (Anhui) Co., Ltd.; Yang Huilai; Mao Jie; Sun Xuexi; (7 pag.)CN106749187; (2017); A;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem