111810-68-5

Basic information

• Product Name: 3-hydroxypyrrolidine hydrochloride
• CAS NO: 111810-68-5
• Molecular Weight: 123.582
• Mol File: 111810-68-5.mol

Chemical Properties

• CAS DataBase Reference: 3-hydroxypyrrolidine hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: 3-hydroxypyrrolidine hydrochloride(111810-68-5)
• EPA Substance Registry System: 3-hydroxypyrrolidine hydrochloride(111810-68-5)

Safety Data

• Hazardous Substances Data: 111810-68-5(Hazardous Substances Data)

Upstream product

• 101469-91-4 (3S)-1-benzyl-3-hydroxypyrrolidine-2,5-dione 
• 101469-92-5 (S)-3-hydroxy-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 127913-44-4 (S)-4-chloro-3-hydroxy butyronitrile 
• 109431-87-0 (R)-tert-butyl 3-hydroxypyrrolidine-1-carboxylate 
• 98-59-9 p-toluenesulfonyl chloride 
• 52334-81-3 2-chloro-5-trifluoromethylpyridine 
• 51-35-4 4R-4-hydroxyproline 
• 130680-56-7 (3R)-N-acetyl-3-(tert-butyldimethylsilyloxy)propylamine 

Downstream Products

• 1315054-87-5 C₇H₁₄N₂O₂ 
• 104641-59-0 (3S)-1-methylpyrrolidin-3-ol 
• 1315054-87-5 C₇H₁₄N₂O₂ 
• 1159816-64-4 1-(5-bromopyridin-2-yl)pyrrolidin-3-ol 
• 1228303-58-9 (3R)-1-{[2-(4-chlorophenyl)-3-(hydroxymethyl)imidazo[1,2-a]pyridin-6-yl]carbonyl}pyrrolidin-3-ol 
• 1072227-55-4 (S)-3-chloro-pyrrolidine hydrochloride 
• 109431-87-0 (R)-tert-butyl 3-hydroxypyrrolidine-1-carboxylate 
• 90512-67-7 3-(R)-hydroxy-1-(N-p-nitrobenzyloxycarbonylacetimidoyl)pyrrolidine 
• 1456714-53-6 1-(2-fluoro-4-iodophenyl)-5-((3-(3-hydroxypyrrolidine-1-carbonyl)phenyl)amino)-3-(4-methoxybenzyl)-6,8-dimethylpyrido[2,3-d]pyrimidine-2,4,7(1H,3H,8H)-trione 
• 1445790-79-3 C₁₇H₁₄F₄N₂O₄S 

Relevant articles and documents

Hydrogenation of chiral nitrile on highly ordered mesoporous carbon-supported Pd catalysts

A highly ordered mesoporous carbon (C-SBA-15 and C-SBA-16) was synthesized by nanocasting method using its corresponding mesoporous silica (SBA-15 and SBA-16) as a template. The obtained porous carbons have high surface areas, large pore volume and a narrow pore size distribution. The N2-adsorption data for C-SBA-15 have provided the BET area of 2029 m2 g-1 and the total pore volume of 1.7 cm3 g-1, and 1637 m2 g-1 and 1.1 cm3 g-1 for C-SBA-16, respectively. The palladium metal impregnated carbon catalysts were employed in the synthesis of (S)-3-pyrrolidinol from chiral (S)-4-chloro-3-hydroxybutyronitrile, and a high yield to (S)-3-pyrrolidinol-salt was obtained by using 1 wt% Pd/C-SBA-16. It was investigated that the well-dispersed Pd metals in the confined mesopores are efficient for the hydrogenation of cyano groups to amine.

Synthesis method of (S)-3-pyrrolidinol hydrochloride

The invention discloses a synthesis method of (S)-3-pyrrolidinol hydrochloride, which belongs to the field of drug synthesis, and comprises the following steps: dehydrating and amidating L-malic acidand benzylamine as raw materials to obtain (3S)-N-benzyl-3-hydroxypyrrolidine-2,5-diketone, and carrying out one-pot reduction, debenzylation and salification to synthesize (S)-3-pyrrolidinol hydrochloride. The method is short in synthetic route, simple to operate, high in yield, good in product purity and beneficial to industrial production.

Preparation method of (S)-3-hydroxypyrrolidine hydrochloride

The invention relates to the field of chemistry, particularly a preparation method of a key intermediate (S)-3-hydroxypyrrolidine hydrochloride of darifenacin for treating overactive bladder syndrome and an antihypertensive drug barnidipine. The preparation method comprises the following steps: carrying out Mitsunobu reaction on (R)-1-N-tert-butyloxycarbonyl-3-hydroxypyrrolidine so as to be condensed with acid to obtain an upturned-structure ester, hydrolyzing ester bond under alkaline conditions to obtain (S)-1-N-tert-butyloxycarbonyl-3-hydroxypyrrolidine, and removing Boc protecting groups under acidic conditions, thereby finally obtaining the key intermediate. The method is simple and easy to implement, has the advantages of cheap and accessible raw materials, lower cost and high yield, and has potential production value.

A PROCESS FOR PREPARATION OF (2S, 5R)-7-OXO-N-[(3S)-PYRROLIDIN-3-YLOXY]-6-(SULFOOXY)-1,6-DIAZABICYCLO [3.2.1]OCTANE-2-CARBOXAMIDE

A process for preparation of a compound of Formula (I) is disclosed.

POLYCYCLIC DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF

Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.

POLYCYCLIC DERIVATIVES, PREPARATION METHOD AND MEDICAL USES THEREOF

Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutical agents, especially the GPR40 agonist and in preparation of drugs for treating diseases like diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.

DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF

The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.

PREPARATION OF DARIFENACIN AND ITS SALTS

Provided are various processes and compounds related to darifenacin and/or its salts. For example, there is provided a process for preparing a free base of darifenacin: Formula, or the salt thereof, the process including reacting 3-(S)-(cyanodiphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-yl) ethyl] pyrrolidine of the Formula (IV), or a salt thereof: Formula (IV) with a base effective to convert the nitrile group of the compound of the Formula (IV) to the amide group of the darifenacin in an organic solvent, the reaction being carried out in the organic solvent, with a proviso that the solvent is not 2-methyl-butan-2-ol, and with further proviso that the reaction produces less than about 0.5 % of the compound of the Formula (Ic): Formula (Ic) in the reaction mass, as measured by HPLC. Various embodiments and variants are provided.

Pteridinone derivatives as PI3-kinases inhibitors

New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.