- PREPARATION METHODE OF 5-PHENYL PENTYL HEXAHYDRO CYCLOPENTAFURAN COMPOUNDS AND CYCLOHEPTANOATE COMPOUNDS
-
A producing method of a 5-phenylpentyl hexahydrocyclopentafuran compound comprises: a step (a) of preparing a 5-phenylfe-1-tenyl hexahydrocyclopentafuran compound which is a compound of chemical formula 1; and a step (b) of producing a 5-phenylpentyl hexahydrocyclopentafuran compound which is a compound of chemical formula 2 by a hydrogenation transition reaction of the compound of chemical formula 1 in the presence of a hydrogenation catalyst, a hydrogen donor and a solvent. In chemical formula 1 and chemical formula 2, R1 is any one selected from a group consisting of hydrogen and hydroxy. The producing method by the present invention enables mass production.COPYRIGHT KIPO 2020
- -
-
Page/Page column 12-13
(2020/04/17)
-
- Process for the preparation of Lubiprostone and intermediates thereof
-
The present invention relates to a novel process for preparing Lubiprostone and novel intermediates prepared from the process. The process of the present invention does not generate hydrogenated by-products that are difficult to be removed, and thus enables the production of Lubiprostone in an efficient and economical way.
- -
-
Page/Page column 24
(2019/11/11)
-
- METHOD OF PRODUCING LUBIPROSTONE
-
PROBLEM TO BE SOLVED: To provide a method allowing efficient production of lubiprostone. SOLUTION: The invention provides a compound represented by the general formula (I) in the figure, where n represents an integer from 0 to 5, and R1 are identical or different and each represent an alkyl group, aralkyl group, aryl group, halogen atom, hydroxy group, alkoxy group, trifluoromethyl group, nitro group, or amino group. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
- -
-
Paragraph 0087
(2019/08/27)
-
- Method for synthesizing 1R,2R,3R-substituted cyclopentanone compound
-
The invention relates to a method for synthesizing a 1R,2R,3R-substituted cyclopentanone compound. The method comprises: carrying out a reaction on a compound 1 and a halogenated alkane in an organicsolvent under the actions of a strong alkali and a cuprous salt to obtain a compound 3, carrying out ester hydrolysis on the compound 3 under the action of an alkali or pancreatin, and carrying out deprotection by using a fluorine reagent to obtain the product. According to the present invention, the synthesis method has characteristics of high yield, high product purity, good diastereoselectivity, easy reaction control and simple post-treatment, is suitable for industrial production, and can synthesize high-purity and high-yield alprostadil, lubiprostone, and the analogs of misoprostol and limaprost. The compound 1 is defined in the specification.
- -
-
Paragraph 0076; 0084-0086
(2018/09/28)
-
- The preparation method of the ruby's forefront
-
The invention relates to a preparation method of lubiprostone, and concretely relates to a preparation method of highly pure lubiprostone represented by formula (I). The method comprises the steps of reducing an initial compound, oxidizing, and hydrolyzing in order to obtain a target compound. Compared with other methods, the method provided by the invention has the advantages of good process reappearance, simple operation, high yield, low cost, high purity of the above obtained product, suitableness for industrialized production, and very high economic benefit.
- -
-
-
- A process for the preparation of intermediates useful in the ruby's forefront, preparation method thereof and through its preparation ruby's forefront method
-
The invention relates to an intermediate for preparing lubiprostone, a preparation method of the intermediate and a method for preparing the lubiprostone through the intermediate, in particular to a compound as shown in a formula V for preparing the lubiprostone (as shown in a formula I), a preparation method of the compound and a method for preparing the lubiprostone through the compound. The method comprises the following steps: performing reduction treatment on the compound as shown in the formula V, performing selective deprotection and hydroxyl oxidation to obtain a compound as shown in a formula II, and performing hydroxyl deprotection on the compound as shown in the formula II to prepare the lubiprostone as shown in the formula I. The method is easy and convenient to operate, high in synthetic yield and suitable for large-scale production.
- -
-
-
- High-purity lubiprostone compound and preparation method thereof
-
The invention belongs to the technical field of medicine, and provides a high-purity lubiprostone compound and a preparation method thereof. According to the method, a LB-2 is taken as a raw material, then is subjected to oxidation and hydrogenation reactions, and then is processed to obtain the high-purity lubiprostone compound, wherein the oxidation reaction employs a dess-martin oxidizing agent, and the hydrogenation reaction is one-step hydrogenation. According to the invention, the production process is simplified, overall yield of the reaction is high, and the high-purity lubiprostone compound is prepared.
- -
-
Paragraph 0031; 0032
(2016/12/26)
-
- Ruby's forefront method for preparing or intermediates (by machine translation)
-
The invention discloses a novel method for preparing a lubiprostone midbody as shown in the formula 7. The method comprises the following steps: (1), a compound as shown in the formula 1 reacts with tert-butyldimethylsilyl chloride to selectively protect a primary hydroxyl group, thereby obtaining a compound shown in the formula 2; (2), a protecting group is applied to the compound 2 under the action of a catalyst, thereby obtaining a compound shown in the formula 3; (3), after the compound 3 is reduced through diisobutylaluminium hydride, a Wittig reaction is carried out on the compound 3, thereby obtaining carboxylic acid shown in the formula 4; (4), the compound 4 is protected in an acetonitrile solvent through a protecting group, thereby obtaining a compound shown in the formula 5; (5), the compound 5 is treated by using the tert-Butyldimethylsilane for removing the protecting group, thereby obtaining a compound shown in the formula 6; and (6), the compound 6 is oxidized by an oxidant and then reacts with a compound shown in the formula (10), thereby obtaining the higher-purity compound shown in the formula 7.
- -
-
Paragraph 0016
(2016/10/08)
-
- PROCESSES FOR PREPARATION OF LUBIPROSTONE
-
PROBLEM TO BE SOLVED: To provide new processes for preparing and purifying lubiprostone. SOLUTION: A process involves 1,4-conjugate addition of a higher order cuprate compound to a protected cyclopentenone intermediate as an important preparation step. Obtained lubiprostone is converted into a guanidine salt derivative that possesses a different melting point and solubility than lubiprostone, and thereby lubiprostone is refined. A novel synthetic intermediate is also present. COPYRIGHT: (C)2015,JPOandINPIT
- -
-
-
- PREPARATION OF LUBIPROSTONE
-
Aspects of the present application relate to process for the preparation of lubiprostone.
- -
-
-
- PROCESSES FOR PREPARATION OF LUBIPROSTONE
-
Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.
- -
-
-
- A LUBIPROSTONE CRYSTAL, ITS PREPARATION PROCESS AND ITS USE
-
A lubiprostone crystal, its preparation process, its pharmaceutical composition or kit, and its use for the preparation of a pharmaceutical composition for treating gastroenteropathy, especial, constipation. The characteristic peaks of 2θ reflection angle in X-ray powder diffraction spectra of the crystal contain 14.6±0.2°, 17.0+0.2° and 19.6±0.2°. The crystal has the advantages of high purity, stable property, and convenient storage and usage compared with amorphous lubisprostone.
- -
-
Page/Page column 6
(2011/02/18)
-
- POLYMORPHIC FORMS OF LUBIPROSTONE
-
There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone.
- -
-
-
- PROCESSES FOR THE PURIFICATION OF LUBIPROSTONE
-
There is provided processes for purification of Lubiprostone by formation of amine salts. Also provided are compounds of the Lubiprostone amine salt. Also provided are compositions comprising Lubiprostone and amines.
- -
-
Page/Page column 16; 17
(2011/07/07)
-
- PROSTAGLANDIN SYNTHESIS AND INTERMEDIATES FOR USE THEREIN
-
Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
- -
-
Page/Page column 5-6
(2010/04/23)
-
- Method for preparing prostaglandin derivative
-
Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.
- -
-
Page/Page column 18
(2010/11/28)
-