73365-02-3

Basic information

• Product Name: N-(TERT-BUTOXYCARBONYL)-D-PROLINAL
• Synonyms: (R)-2-FORMYL-PYRROLIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER;(R)-(+)-1-BOC-2-PYRROLIDINECARBALDEHYDE;(R)-N-BOC-PROLINAL;N-(TERT-BUTOXYCARBONYL)-D-PROLINAL;N-T-BOC-D-PROLINAL;BOC-D-PROLINAL;(R)-2-FORMYL-PYRROLIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER (R)-N-BOC-PROLINAL;(R)-N-BOC-PROLINAL, 97+%
• CAS NO: 73365-02-3
• Molecular Formula: C₁₀H₁₇NO₃
• Molecular Weight: 199.25
• EINECS: 1312995-182-4
• Product Categories: Amino Aldehydes;Amino Acid Derivatives;Peptide Synthesis
• Mol File: 73365-02-3.mol
• Article Data: 40

Chemical Properties

• Boiling Point: 228 °C(lit.)
• Flash Point: >230 °F
• Appearance: Colorless to yellow/Liquid
• Density: 1.059 g/mL at 25 °C(lit.)
• Vapor Pressure: 0.005mmHg at 25°C
• Refractive Index: n20/D 1.461(lit.)
• Storage Temp.: Freezer (-20°C)
• PKA: -3.03±0.40(Predicted)
• Sensitive: Air Sensitive
• CAS DataBase Reference: N-(TERT-BUTOXYCARBONYL)-D-PROLINAL(CAS DataBase Reference)
• NIST Chemistry Reference: N-(TERT-BUTOXYCARBONYL)-D-PROLINAL(73365-02-3)
• EPA Substance Registry System: N-(TERT-BUTOXYCARBONYL)-D-PROLINAL(73365-02-3)

Safety Data

• Hazard Codes: Xi
• Statements: 36/37/38
• Safety Statements: 26-36
• WGK Germany: 3
• Hazardous Substances Data: 73365-02-3(Hazardous Substances Data)

Usage

Chemical Properties

Clear colorless to yellow liquid

InChI:InChI=1/C10H17NO3/c1-10(2,3)14-9(13)11-6-4-5-8(11)7-12/h7-8H,4-6H2,1-3H3

Upstream product

• 43041-12-9 methyl (2R)-pyrrolidine-2-carboxylate 
• 201230-82-2 carbon monoxide 
• 73286-71-2 N-(tert-butoxycarbonyl)-2,3-dihydropyrrole 
• 344-25-2 D-Prolin 
• 6216-63-3 N-Cbz-Prolinol 
• 59378-81-3 1-(tert-butoxycarbonyl)prolin-2R-ol 
• 79-37-8 oxalyl dichloride 
• 852324-75-5 (2R)-N-Boc-prolinethioester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 68832-13-3 D-prolinol 
• 288086-98-6 [tert-butyl (R)-2-(methoxy(methyl)carbamoyl)pyrrolidine-1-carboxylate] 
• 73323-65-6 1-(tert-butyl) 2-methyl (R)-pyrrolidine-1,2-dicarboxylate 
• 549531-94-4 (2R)-1-(tert-butoxycarbonyl)-2-[(tert-butyldimethylsilyl)oxymethyl]pyrrolidine 

Downstream Products

• 1201581-83-0 tert-butyl (R)-2-[(3-fluorophenylamino)methyl]pyrrolidine-1-carboxylate 
• 1201580-77-9 6-{(R)-2-[(E)-2-(3-chlorophenyl)vinyl]pyrrolidin-1-yl}-9H-purine 
• 1201581-84-1 tert-butyl (R)-2-{[(3-fluorophenyl)methylamino]methyl}pyrrolidine-1-carboxylate 
• 1201581-98-7 (R)-2-[(E)-2-(3-chlorophenyl)vinyl]pyrrolidine 
• 1201581-96-5 (3-fluorophenyl)-(R)-1-pyrrolidin-2-ylmethylamine 
• 1201580-73-5 (3-fluorophenyl)-[(R)-1-(9H-purin-6-yl)pyrrolidin-2-ylmethyl]amine 
• 1201581-97-6 C₁₂H₁₇FN₂ 
• 1201580-75-7 (3-fluorophenyl)methyl-[(R)-1-(9H-purin-6-yl)pyrrolidin-2-ylmethyl]amine 
• 1201581-85-2 tert-butyl (R)-2-[(E)-2-(3-chlorophenyl)vinyl]pyrrolidine-1-carboxylate 
• 1223386-86-4 tert-butyl (2R)-2-[hydroxy(phenyl)methyl]pyrrolidine-1-carboxylate 
• 1369427-40-6 (2R,3R)-3-((S)-1-(tert-butoxycarbonyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropionic acid dicyclohexylamine salt 
• 440361-71-7 R-pyrrolidine-2-carbaldehyde 

Relevant articles and documents

X-ray Structure-Guided Discovery of a Potent, Orally Bioavailable, Dual Human Indoleamine/Tryptophan 2,3-Dioxygenase (hIDO/hTDO) Inhibitor That Shows Activity in a Mouse Model of Parkinson’s Disease

Human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) have been closely linked to the pathogenesis of Parkinson’s disease (PD); nevertheless, development of dual hIDO1 and hTDO inhibitors to evaluate their potential efficacy against PD is still lacking. Here, we report biochemical, biophysical, and computational analyses revealing that 1H-indazole-4-amines inhibit both hIDO1 and hTDO by a mechanism involving direct coordination with the heme ferrous and ferric states. Crystal structure-guided optimization led to23, which manifested IC50values of 0.64 and 0.04 μM to hIDO1 and hTDO, respectively, and had good pharmacokinetic properties and brain penetration in mice.23showed efficacy against the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse motor coordination deficits, comparable to Madopar, an anti-PD medicine. Further studies revealed that different from Madopar,23likely has specific anti-PD mechanisms involving lowering IDO1 expression, alleviating dopaminergic neurodegeneration, reducing inflammatory cytokines and quinolinic acid in mouse brain, and increasing kynurenic acid in mouse blood.

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