Abstract: The present invention relates to kinetic resolution of racemic ?-hydroxyl ester via asymmetric catalytic hydrogenation and an application thereof. In the presence of chiral spiro pyridyl phosphine ligand Iridium catalyst and base, racemic ?-hydroxyl esters were subjected to asymmetric catalytic hydrogenation to obtain extent optical purity chiral ?-hydroxyl esters and corresponding 1,5-diols. An optically active chiral ?-hydroxyl ester and 1,5-diols can be obtained at very high enantioselectivity and yield with relatively low usage of catalyst. The chiral ?-hydroxyl ester and 1,5-diols obtained by using the method can be used as a critical raw material for asymmetric synthesis of chiral drugs (R)-lisofylline and natural drugs (+)-civet, (?)-indolizidine 167B and (?)-coniine.

Abstract: The present invention relates to the technical field of ibrutinib, particularly to the technical field of ibrutinib intermediate compounds and preparation methods thereof. The intermediate compounds are represented by formula A, wherein, the dotted line represents a double bond or a single bond between carbon and oxygen.

Abstract: The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R1 or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.

Abstract: A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes: reacting a compound of formula I below with a compound of formula II in the presence of an organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf)3 to prepare a compound of formula III below: wherein R1 is alkyl, phenyl or benzyl; R2, R3, R4 are each independently C1-C6 alkyl or C6-C10 aryl; the chiral amine oxide L has the following structure: wherein n=1, 2; and R=Ph—, 2,6—Me2C6H3—, 2,6—Et2C6H3—, 2,6-iPr2C6H3—, Ph2CH—.

Abstract: The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone.

Abstract: The present invention relates to the technical field of medicine and organic synthesis, particularly to a method for preparing crizotinib. The method comprises the compound of formula b and the compound of formula e undergoing Suzuki coupling reaction to produce the compound of formula a which then was subjected to deprotection to afford (±) crizotinib.

Abstract: Disclosed are a silodosin intermediate and a preparation method thereof. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromide and R1 is hydrogen. The formyl group may be a group having the structure shown by the formula I. R7 is a protecting group of carboxyl, and R2 is 3-hydroxypropyl or a group having the structure shown by the formula II. W is a protecting group of hydroxyl. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%.

Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.

Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.

Abstract: The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R1, R2, R3, R4, R5, R6, R7, R8 and R9 having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7?-diarylphosphino-1,1?-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.

Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.

Abstract: The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R1, R2, R3, R4, R5, R6, R7, R8 and R9 having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7?-diarylphosphino-1,1?-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.

Abstract: Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro bromobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.

Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.

Abstract: Disclosed is a preparation method of ?-imatinib mesylate. The reaction temperature of the method is low and the yield of the crystal is improved. Furthermore, the method is applicable to the industrial production.

Abstract: The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin.

Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.

Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.