Shanghai Institute of Pharmaceutical Industry

Zhejiang Hisun Pharmaceutical Co., Ltd.

China State Institute of Pharmaceutical Industry

China National Medicines Guorui Pharmaceutical Co., Ltd.

Zhejiang Kangyu Pharmaceutical Co., Ltd.

Fuli Zhang

Hua Bai

Zhezhou Yang

Rusheng Bao

Meihua Xie

Pengcheng Qiu

Chunbo Yang

Weiwei Xu

Jian Chai

Bin Liang

Qingfeng Cai

Daoxin Chen

Rentong Sun

Meng Hu

Taizhi Wu

Chonghao Liu

Yang Gao

Zhiqing Yang

Jiang Li

Jian Wang

Hairong Luo

Lizhi Zhao

Jialiang Zhong

Linyong Jin

Hu Pan

Linyu Pan

Dongming Jiang

Min Jiang

Anping Lai

Mengya Ge

The present invention discloses a salt derivative of 1-(3-methanesulfonamidobenzyl)-6-methoxy-7-benzyloxy-1,2,3,4-tetrahydroisoquinoline. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL.

Salt derivative of tetrahydroisoquinoline and crystalline thereof and preparation method therefore and application thereof

Intermediate compounds for the preparation of Praziquantel are provided. In particular, the intermediate compounds provided include a compound of formula (IV) and a compound of formula (V). Also provided are processes for preparing the intermediate compounds. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound Praziquantel is high, so that industrialized mass production of Praziquantel using the intermediate compounds is easy to achieve.

Intermediate compounds for preparation of praziquantel and processes for preparing the intermediate compounds

Disclosed is a preparation method for praziquantel and intermediates thereof. The method includes: obtaining a target product praziquantel by using &#x3b2;-phenethylamine as an initial raw material through a condensation reaction with chloroacetyl chloride, a substitution reaction with ethanolamine, and an acylation reaction with cyclohexanecarbonyl chloride, followed by an oxidation reaction and cyclization reaction. Also disclosed are two key intermediates, namely, a compound of formula IV and a compound of formula V for preparing praziquantel. The preparation method is reasonable and simple in its technological design, uses moderate reaction conditions, and is economical and environmentally friendly. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound praziquantel is high, so that industrialized mass production is easy to achieve.

Preparation method for praziquantel and intermediate compounds thereof

A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof. 

4-substituent-2-hydroxylmorpholine-3-one and preparation method thereof

The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity. 

4-benzyl-1-phenethyl-piperazine-2,6-dione preparation method, and intermediate and preparation method thereof

Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. 

Method for preparing linezolid intermediate

The present invention provides a preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate, preparation methods for intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium, (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium, as well as a method for using (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium to prepare rivastigmine which can be used for the treatment of Alzheimer's disease.

Preparation method for rivastigmine, intermediates thereof, and preparation method for said intermediates

A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20&#xb0; C. to 60&#xb0; C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.

Method for preparing rivaroxaban intermediate

The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole, or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole.

Process for the preparation of 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylates

The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N&#x2014;[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.

Preparation method of rivastigmine, its intermediates and preparation method of the intermediates

A new method of preparing memantine hydrochloride, comprising the following steps: reacting 1-bromo-3,5-dimethyl adamantane and urea/formic acid, with formic acid also acting as the solvent; hydrolyzing with aqueous inorganic acid; alkalifying, extracting and acidifying with hydrochloric acid; finally collecting target compound. The method uses inexpensive raw materials and is performed in homogeneous phase under mild conditions. It can achieve high yield and good product purity, and is suitable for macrochemistry. The purity of crude product is 99.0%, and reaches 99.98% after first recrystallization, yield: 69.5%, mp: 332 C (DSC).

Method of preparing memantine hydrochloride

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Shanghai, China

Fuli Zhang