Abstract: The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.

Abstract: The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof.

Abstract: The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation.

Abstract: The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof.

Abstract: The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

Abstract: Disclosed are aminosulfonyl-based compounds represented by the general formula I or tautomers, enantiomers, racemates or pharmaceutically acceptable salts thereof, a method for preparing the same, pharmaceutical compositions and uses thereof. The compounds can be used to treat epilepsy, convulsions, obesity and the like.

Abstract: The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.

Abstract: This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.

Abstract: The present invention relates to a (2R,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.

Abstract: Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof.

Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.

Abstract: Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof.

Abstract: The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia.

Abstract: The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity.

Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III and utilized for preparing vardenafil), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound.

Abstract: A method for preparing 3?-arachidylamido-7?,12?,5?-cholan-24-carboxylic acid represented by the following formula V is disclosed, which includes the following steps: converting cholic acid to the compound of formula III by acylation reaction and azidation reaction, reducing the compound of formula III to the compound of formula IV and in the end acylating the compound of formula IV with arachidoyl chloride to get the compound of formula V. The method avoids the use of protection groups.

Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.

Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.

Abstract: The present invention discloses a process for preparing sildenafil and its intermediates having the structures outlined below: In particular, the present invention provides a process for preparing the compound of formula (I) and its intermediates, i.e. the compounds of formula (I), (II), (III) and (IV). The compound of formula (I) is obtained from the compound of formula (II); the compound (II) is obtained from the compound of formula (III) and methylpiperazine; the compound (III) is obtained by treating the compound of formula (IV) with chlorosulfonic acid; the compound (IV) is obtained though treating the compound of formula (V) in the presence of at least one selected from POX3, PX3, PX5 and their mixtures in any ratio. The process for preparing the compound of formula (I) according to the present invention reduces the side reactions in the processes of the prior art. These improvements lead to higher yields and a better industrial applicability with easier controlling of the reaction.

Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure.