The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.

The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.

Provided is a continuous synthesis method for 1,1′-bicyclic[1.1.1]pentane-1,3-diethyl ketone compounds. The continuous synthesis method comprises: under the irradiation of a light source, continuously conveying raw material A and raw material B to a continuous reaction device for a continuous photochemical reaction to obtain 1,1′-bicyclic[1.1.1]pentane-1,3-diethyl ketone compounds, and controlling the reaction temperature in the continuous reaction device by a temperature control device during the continuous photochemical reaction. A propellane with substituents, as a reaction raw material, is subjected to the above photochemical reaction in the continuous reaction device to reduce the probability of its slow decomposition and deterioration under the irradiation, and greatly improve the conversion rate of the reaction material and product yield.

Provided is a continuous synthesis method for 1,1′-bicyclic[1.1.1]pentane-1,3-diethyl ketone compounds. The continuous synthesis method comprises: under the irradiation of a light source, continuously conveying raw material A and raw material B to a continuous reaction device for a continuous photochemical reaction to obtain 1,1′-bicyclic[1.1.1]pentane-1,3-diethyl ketone compounds, and controlling the reaction temperature in the continuous reaction device by a temperature control device during the continuous photochemical reaction. A propellane with substituents, as a reaction raw material, is subjected to the above photochemical reaction in the continuous reaction device to reduce the probability of its slow decomposition and deterioration under the irradiation, and greatly improve the conversion rate of the reaction material and product yield.

The present invention provides a process for preparing a dimethylcyclobutane compound of the following general formula (1A), the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2) with a phosphonic ester compound of the following general formula (3) to produce an unsaturated ester compound of the following general formula (4), having a dimethylcyclobutane ring, and subjecting the unsaturated ester compound (4), having a dimethylcyclobutane ring, to a reduction reaction to produce the dimethylcyclobutane compound (1A).

##STR00001##

The present invention provides a process for preparing a dimethylcyclobutane compound of the following general formula (1A), the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2) with a phosphonic ester compound of the following general formula (3) to produce an unsaturated ester compound of the following general formula (4), having a dimethylcyclobutane ring, and subjecting the unsaturated ester compound (4), having a dimethylcyclobutane ring, to a reduction reaction to produce the dimethylcyclobutane compound (1A). ##STR00001##

The present invention provides a process for preparing a dimethylcyclobutane compound of the following general formula (1A), the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2) with a phosphonic ester compound of the following general formula (3) to produce an unsaturated ester compound of the following general formula (4), having a dimethylcyclobutane ring, and subjecting the unsaturated ester compound (4), having a dimethylcyclobutane ring, to a reduction reaction to produce the dimethylcyclobutane compound (1A). ##STR00001##

The invention relates to compositions and methods for inhibiting Krüppel-like Factor 10 (KLF10) for modulation of T regulatory cells and cancer immunotherapy.

The present invention provides a process for preparing a dimethylcyclobutane compound of the following general formula (1A), the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2) with a phosphonic ester compound of the following general formula (3) to produce an unsaturated ester compound of the following general formula (4), having a dimethylcyclobutane ring, and subjecting the unsaturated ester compound (4), having a dimethylcyclobutane ring, to a reduction reaction to produce the dimethylcyclobutane compound (1A).

##STR00001##

The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.