1499-56-5

Usage

Uses

Used in Pharmaceutical Industry:
TRANS-4-HYDROXY-L-PROLINE METHYL ESTER is used as a key intermediate in the synthesis of various pharmaceutical compounds, particularly in the preparation of Pyridazinamine derivatives. These derivatives act as modulators of SMARCA2 and BRM target proteins, which play crucial roles in the regulation of gene expression and cellular processes. By modulating these target proteins, Pyridazinamine derivatives have the potential to treat various diseases and disorders related to the dysregulation of these proteins.
Used in Chemical Synthesis:
TRANS-4-HYDROXY-L-PROLINE METHYL ESTER is also used as a versatile building block in the synthesis of various organic compounds, including natural products, pharmaceuticals, and agrochemicals. Its unique chemical structure allows for a wide range of reactions, such as esterification, amidation, and cyclization, making it a valuable starting material for the development of new molecules with diverse applications.

InChI:InChI=1/C6H11NO3/c1-10-6(9)5-2-4(8)3-7-5/h4-5,7-8H,2-3H2,1H3/t4?,5-/m0/s1

Upstream product

• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 67-56-1 methanol 
• 2584-71-6 cis-hydroxy-D-proline 
• 3398-22-9 trans-4-hydroxyproline 
• 75-36-5 acetyl chloride 
• 51-35-4 4R-4-hydroxyproline 
• 1063998-64-0 (2S,4R)-4-Hydroxy-pyrrolidine-2-carbonyl chloride 
• 60-29-7 diethyl ether 
• 186581-53-3 diazomethane 

Downstream Products

• 90965-82-5 Phe-Hyp 
• 61703-38-6 trans-4-hydroxy-L-proline amide 
• 64187-48-0 methyl (2S,4R)-1-benzyloxycarbonyl-4-hydroxypyrrolidine-2-carboxylate 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 5211-24-5 (2S)-2,5-dihydro-1H-pyrrole-1,2-dicarboxylic acid 2-methyl 1-(phenylmethyl) ester 
• 31560-20-0 (2S,4R)-1-benzoyl-4-hydroxypyrrolidine-2-carboxylic acid methyl ester 
• 80514-79-0 trans-N-trityl-4-hydroxy-L-proline 
• 129430-93-9 methyl (2S,4R)-4-hydroxy-1-tritylpyrrolidine-2-carboxylate 
• 791060-66-7 ((2S,4S)-4-fluoropyrrolidin-2-yl)methanol 
• 317356-27-7 tert-butyl (2S,4S)-4-fluoro-2-(hydroxymethyl)pyrrolidine-1-carboxylate 
• 882990-58-1 (2S,4R)-2-{1-benzyl-4-[(triisopropylsilyl)oxy]-pyrrolidinyl}methanol 
• 882990-54-7 (2S,4R)-methyl 1-benzyl-4-((triisopropylsilyl)oxy)pyrrolidine-2-carboxylate 
• 882990-56-9 (2S,4R)-2-{1-benzyl-4-[(tert-butyldiphenylsilyl)oxy]-pyrrolidinyl}methanol 
• 882990-52-5 (2S,4R)-1-benzyl-4-[(tert-butyldiphenylsilyl)oxy]-2-methoxycarbonylpyrrolidine 

Relevant academic research and scientific papers

BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY

The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

As Aurora kinase inhibitor derivatives

The present invention relates to a substituted pyrazole derivative used for inhibiting Aurora kinase and represented by formula (I) or formula (Ia), or stereo isomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, esters, pharmaceutically acceptable salts or prodrugs thereof, a medicinal composition containing the above compounds as active ingredients, and a use of the compounds and the medicinal composition in preparation of medicines for protecting, processing, treating or mitigating proliferative diseases of patients.

Pyrrolidine ring puckering and prolyl amide bond configurations of 2-methyl-allo-hydroxyproline-based dipeptides

An expeditious method for the synthesis of homo and heterochiral dipeptides containing l-alanine and d/l 2-methyl allo-hydroxyl prolines was developed using direct aminolysis of bicyclic lactones derived from d/l alanine. The impact of C-2 methylation and its spatial orientation on the pyrrolidine ring puckering and prolyl amide bond configuration was ascertained by solution NMR studies. The present studies reveal that C-2 methylation causes the prolyl amide bond to exist exclusively in the trans geometry in both homo- and heterochiral dipeptides. However, the spatial orientation of the C-2 methyl group and its i + 2 position in appropriately capped model dipeptides may nucleate into a turn like structure.

CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE

Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.

Synthesis method of teneligliptin key intermediate

The invention discloses a synthesis method of a teneligliptin key intermediate, and relates to the technical field of synthesis, in particular to a synthesis method of a teneligliptin key intermediate(2S)-4-oxo-2-(3-thiazolidinylcarbonyl)-1-pyrrolidinecarboxylic acid tert-butyl ester. According to the synthesis method, L-hydroxyproline is subjected to an esterification reaction to obtain a compound 1; the compound 1 is protected by t-butyloxycarboryl to obtain a compound 2; the compound 2 is subjected to an oxidation reaction to obtain a compound 3; the compound 3 and thiazolidine are subjected to an ammonia ester exchange reaction to obtain a compound 4. According to the method, a synthesis route suitable for industrial production is designed aiming at the teneligliptin key intermediate,the complexity of the operation is lowered, expensive dehydration reagents are also avoided, the yield is high, the cost is low, and the synthesis method is suitable for industrial application and popularization.

As Aurora kinase inhibitors of the substituted quinazoline derivatives

The invention relates to a substituted quinazoline derivative as an aurora kinase inhibitor, which is shown as structural formula (I) or (Ia), tautomers, hydrates, solvates or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the tautomers, hydrates, solvates and pharmaceutically acceptable salts as drug active ingredients, and application of the compounds and the pharmaceutical compositions in preparation of medicines for protection, treatment, curing or alleviation of proliferative diseases of patients.

Substituted pyridine compound and its method and use thereof

The invention relates to a novel substitutive pyridine compound, and a pharmaceutically acceptable salt and a pharmaceutical preparation of the substitutive pyridine compound for regulating the activity of protein kinases and regulating signal responses between cells or in the cells. Meanwhile, the invention further relates to a pharmaceutical composition containing the compound provided by the invention, and a method for treating high proliferative diseases of mammals, especially human with the pharmaceutical composition.

SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF

Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

CONJUGATION LINKERS, CELL BINDING MOLECULE-DRUG CONJUGATES CONTAINING THE LIKERS, METHODS OF MAKING AND USES SUCH CONJUGATES WITH THE LINKERS

The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.

N-methyl-D-aspartate receptor modulators and methods of making and using same

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.