135065-76-8

Basic information

• Product Name: (S)-N-Boc-2-Hydroxymethylmorpholine
• Synonyms: (S)-2-Hydroxymethylmorpholine-4-carboxylic acid tert-butyl ester;N-Boc-(S)-3-morpholine-methanol;(S)-N-BOC-2-HYDROXYMETHYLMORPHOLINE;(S)-4-BOC-2-HYDROXYMETHYL-MORPHOLINE;(2S)-2-hydroxymethyl-morpholine-4-carboxylic acid tert-butyl ester;(S)-N-Boc-2-HydroxyMethyl...;tert-Butyl (2S)-2-(hydroxyMethyl)Morpholine-4-carboxylate;4-Morpholinecarboxylic acid, 2-(hydroxyMethyl)-, 1,1-diMethylethyl ester, (2S)-
• CAS NO: 135065-76-8
• Molecular Formula: C₁₀H₁₉NO₄
• Molecular Weight: 217.26
• EINECS: 1312995-182-4
• Product Categories: pharmacetical;API intermediates;Heterocycle-other series
• Mol File: 135065-76-8.mol
• Article Data: 20

Chemical Properties

• Melting Point: 60-62 °C
• Boiling Point: 321 °C
• Flash Point: 148 °C
• Appearance: White crystal powder
• Density: 1.118
• Vapor Pressure: 2.53E-05mmHg at 25°C
• Refractive Index: 1.474
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: 14.36±0.10(Predicted)
• Water Solubility: Slightly soluble in water.
• Sensitive: Light Sensitive
• CAS DataBase Reference: (S)-N-Boc-2-Hydroxymethylmorpholine(CAS DataBase Reference)
• NIST Chemistry Reference: (S)-N-Boc-2-Hydroxymethylmorpholine(135065-76-8)
• EPA Substance Registry System: (S)-N-Boc-2-Hydroxymethylmorpholine(135065-76-8)

Safety Data

• Hazardous Substances Data: 135065-76-8(Hazardous Substances Data)

Usage

Uses

(S)-N-Boc-2-hydroxymethylmorpholine is used as a pharmaceutical intermediate.

InChI:InChI=1/C10H19NO4/c1-10(2,3)15-9(13)11-4-5-14-8(6-11)7-12/h8,12H,4-7H2,1-3H3/t8-/m0/s1

Upstream product

• 167357-55-3 (+)-2(S)-(phenylmethyloxymethyl)morpholine 
• 868689-63-8 (S)-2,4-morpholinedicarboxylic acid 4-(1,1-dimethylethyl)ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 847805-30-5 (6S)-6-(hydroxymethyl)morpholin-3-one 
• 911223-10-4 (S)-2-benzyloxymethyl-morpholine-4-carboxylic acid tert-butyl ester 
• 135065-72-4 (S)-N-benzyl-3-chloroacetamidopropane-1,2-diol 
• 148638-78-2 (S)-4-Benzyl-6-hydroxymethyl-morpholin-3-one 
• 148638-77-1 N-Benzyl-2-chloro-N-((S)-2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-acetamide 
• 132073-82-6 (S)-4-Benzyl-2-(hydroxymethyl)morpholine 
• 847805-29-2 (-)-2-chloro-N-((S)-2,3-dihydroxypropyl)acetamide 
• 132073-83-7 (S)-morpholin-2-ylmethanol 

Downstream Products

• 859205-93-9 (S)-2-{4-[3-chloro-4-(3-fluoro-benzyloxy)-5 phenylamino]-pyrrolo[2,1-f][1,2,4]triazin-5-ylmethoxy methyl}-morpholine-4-carboxylic acid tert-butyl ester 
• 1159598-72-7 (2S)-[4-(4-fluoro-phenyl)-piperazine-1-carbonyloxymethyl]-morpholine-4-carboxylic acid tert-butyl ester 
• 1159598-94-3 (2S)-[4-(2,4-difluoro-phenyl)-piperazine-1-carbonyloxymethyl]-morpholine-4-carboxylic acid tert-butyl ester 
• 1159598-59-0 (2S)-(4-phenylpiperazine-1-carbonyloxymethyl)-morpholine-4-carboxylic acid tert-butyl ester 
• 500702-97-6 benzyl (2S)-2-(hydroxymethyl)morpholine-4-carboxylate 
• 259180-69-3 tert-butyl (2R)-2-(cyanomethyl)morpholine-4-carboxylate 
• 1137478-34-2 (R)-tert-butyl 2-((2-(5-cyanopyrazin-2-ylamino)-5-(4-methoxyphenyl)pyridin-4-ylamino)methyl)morpholine-4-carboxylate 

Relevant articles and documents

Radiosynthesis and evaluation of 18F-labeled dopamine D4-receptor ligands

Introduction: The dopamine D4 receptor (D4R) has attracted considerable attention as potential target for the treatment of a broad range of central nervous system disorders. Although many efforts have been made to improve the performance of putative radioligand candidates, there is still a lack of D4R selective tracers suitable for in vivo PET imaging. Thus, the objective of this work was to develop a D4-selective PET ligand for clinical applications. Methods: Four compounds based on previous and new lead structures were prepared and characterized with regard to their D4R subtype selectivity and predicted lipophilicity. From these, 3-((4-(2-fluorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine I and (S)-4-(3-fluoro-4-methoxybenzyl)-2-(phenoxymethyl)morpholine II were selected for labeling with fluorine-18 and subsequent evaluation by in vitro autoradiography to assess their suitability as D4 radioligand candidates for in vivo imaging. Results: The radiosynthesis of [18F]I and [18F]II was successfully achieved by copper-mediated radiofluorination with radiochemical yields of 7% and 66%, respectively. The radioligand [18F]II showed specific binding in areas where D4 expression is expected, whereas [18F]I did not show any uptake in distinct brain regions and exhibited an unacceptable degree of non-specific binding. Conclusions: The compounds studied exhibited high D4R subtype selectivity and logP values compatible with high brain uptake, but only ligand [18F]II showed low non-specific binding and is therefore a good candidate for further evaluation. Advances in knowledge: The discovery of new lead structures for high-affinity D4 ligands opens up new possibilities for the development of suitable PET-radioligands. Implications for patient: PET-imaging of dopamine D4-receptors could facilitate understanding, diagnosis and treatment of neuropsychiatric and neurodegenerative diseases.

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