990-91-0

Basic information

• Product Name: Tetrabenzyl pyrophosphate
• Synonyms: PYROPHOSPHORIC ACID TETRABENZYL ESTER;TETRABENZYL PYROPHOSPHATE;TETRABENZYL DIPHOSPHATE;Tetrabenzyl pyrophosphate, tech.;Pyrophosphoric acid tetrabenzyl ester, Tetrabenzyl diphosphate;Bis(phenylmethoxy)phosphoryl bis(phenylmethyl) phosphate;Tetrabenzyl yrophosphate;Benzyl Pyrophosphate
• CAS NO: 990-91-0
• Molecular Formula: C₂₈H₂₈O₇P₂
• Molecular Weight: 538.47
• EINECS: 1312995-182-4
• Product Categories: Biochemistry;Nucleosides, Nucleotides & Related Reagents;Phosphorylating and Phosphorothioating Agents;Phosphorylation;Protecting Agents, Phosphorylating Agents & Condensing Agents;Synthetic Organic Chemistry;Phosphorylating and Phosphitylating Agents
• Mol File: 990-91-0.mol
• Article Data: 15

Chemical Properties

• Melting Point: 63-66 °C(lit.)
• Boiling Point: 601.6 °C at 760 mmHg
• Flash Point: 330.4 °C
• Appearance: White to off-white/Powder or Crystalline Powder
• Density: 1.289 g/cm³
• Vapor Pressure: 8.62E-14mmHg at 25°C
• Refractive Index: 1.59
• Storage Temp.: −20°C
• Water Solubility: Slightly soluble in water.
• Sensitive: Moisture Sensitive
• BRN: 2068292
• CAS DataBase Reference: Tetrabenzyl pyrophosphate(CAS DataBase Reference)
• NIST Chemistry Reference: Tetrabenzyl pyrophosphate(990-91-0)
• EPA Substance Registry System: Tetrabenzyl pyrophosphate(990-91-0)

Safety Data

• Hazard Codes: C
• Statements: 34
• Safety Statements: 26-36/37/39-45
• RIDADR: UN 3261 8/PG 2
• WGK Germany: 3
• F: 10-21
• HazardClass: 8
• PackingGroup: II
• Hazardous Substances Data: 990-91-0(Hazardous Substances Data)

Usage

Chemical Properties

White Solid

Uses

Tetrabenzyl pyrophosphate is used in the preparation of phosphoryl derivatives of shikimic acid in the presence of LDA. It is used in the preparation of dibenzyl phosphoro fluoridate in the presence of cesium fluoride as a catalyst. It is also used as a precursor in pharmaceuticals and involved in the phosphorylation of inositol derivatives.

InChI:InChI=1/C28H28O7P2/c29-36(31-21-25-13-5-1-6-14-25,32-22-26-15-7-2-8-16-26)35-37(30,33-23-27-17-9-3-10-18-27)34-24-28-19-11-4-12-20-28/h1-20H,21-24H2

Synthetic route

phosphoric acid dibenzyl ester (1623-08-1) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
With dicyclohexyl-carbodiimide In Isopropyl acetate at 0 - 6℃; for 1.5h; Inert atmosphere;	96%
With N,N-dicyclohexylurea In toluene at 20℃; for 5h;	95%
With dicyclohexyl-carbodiimide In Isopropyl acetate at 3℃; for 0.916667 - 1.08333h;	91%

Dibenzyl phosphite (17176-77-1) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
With N,N,N,N,-tetramethylethylenediamine; copper(ll) bromide In tetrahydrofuran at 25℃; for 15h;	90%
With tetrachloromethane; N-benzyl-N,N,N-triethylammonium chloride; potassium carbonate In toluene at 60℃; for 0.5h;	88%
With N-chloro-succinimide; benzene anschliessendes Behandeln mit Phosphorsaeure-dibenzylester und Triaethylamin;

1.3-butanediol (18826-95-4, 107-88-0) + tribenzyl phosphite (15205-57-9) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + dibenzyl hydrogen phosphite (538-60-3) + 3-(dibenzyl)phosphoryloxy-1-methyl-1-propanol (123417-01-6)

Conditions	Yield
Stage #1: tribenzyl phosphite With iodine In dichloromethane at 0 - 20℃; for 0.416667h; Stage #2: 1.3-butanediol With pyridine In dichloromethane at 20℃; for 0.5h;	A n/a B n/a C 65%

pyridine (110-86-1) + phosphoric acid dibenzyl ester (1623-08-1) + p-toluenesulfonyl chloride (98-59-9) + benzene (71-43-2) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

pyridine (110-86-1) + phosphoric acid dibenzyl ester (1623-08-1) + 4-Nitrobenzenesulfonyl chloride (98-74-8) + benzene (71-43-2) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

tetrachloromethane (56-23-5) + Dibenzyl phosphite (17176-77-1) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
With potassium hydroxide

Bromotrichloromethane (75-62-7) + Dibenzyl phosphite (17176-77-1) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
With potassium hydroxide

dibenzyl phosphochloridate (538-37-4) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
With potassium hydroxide

phosphoric acid dibenzyl ester (1623-08-1) + triethylamine (121-44-8) + acetonitrile (75-05-8) + trifluoroacetic anhydride (407-25-0) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

tetrachloromethane (56-23-5) + Dibenzyl phosphite (17176-77-1) + aqueous KOH → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Bromotrichloromethane (75-62-7) + Dibenzyl phosphite (17176-77-1) + aqueous KOH → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

dibenzyl phosphochloridate (538-37-4) + aqueous KOH → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

N,N-diethylaniline (91-66-7) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
Multi-step reaction with 2 steps 1: benzene; PCl3 / 5 °C / anschliessendes Behandeln mit Wasser 2: aqueous KOH View Scheme
Multi-step reaction with 2 steps 1: benzene; PCl3 / 5 °C / anschliessendes Behandeln mit Wasser 2: aqueous KOH View Scheme

benzyl alcohol (100-51-6) → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
Multi-step reaction with 2 steps 1: benzene; PCl3 / 5 °C / anschliessendes Behandeln mit Wasser 2: aqueous KOH View Scheme
Multi-step reaction with 2 steps 1: benzene; PCl3 / 5 °C / anschliessendes Behandeln mit Wasser 2: aqueous KOH View Scheme

benzyl alcohol (100-51-6) + sodium → dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0)

Conditions	Yield
Multi-step reaction with 2 steps 1: H3PO4, Et3N, trichloroacetonitrile 2: DCC View Scheme

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 1-O-(tert-butyldimethylsilyl)-3-(2-hydroxy-4,6-dimethylphenyl)-3,3-dimethylpropan-1-ol (134098-64-9) → dibenzyl (2-(4-((tert-butyldimethylsilyl)oxy)-2-methylbutan-2-yl)-3,5-dimethylphenyl) phosphate (153910-63-5)

Conditions	Yield
Stage #1: 1-O-(tert-butyldimethylsilyl)-3-(2-hydroxy-4,6-dimethylphenyl)-3,3-dimethylpropan-1-ol With potassium tert-butylate In tetrahydrofuran at 60℃; for 0.0833333h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at 60℃; for 1h;	100%
With potassium tert-butylate In tetrahydrofuran at 60℃; for 0.75h;	87%
Stage #1: 1-O-(tert-butyldimethylsilyl)-3-(2-hydroxy-4,6-dimethylphenyl)-3,3-dimethylpropan-1-ol With potassium tert-butylate In tetrahydrofuran at 60℃; for 0.0833333h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran for 1h; Reflux;	87.2%
With potassium tert-butylate In tetrahydrofuran at 60℃;	43.8%
In N,N-dimethyl-formamide; mineral oil

1-O-benzyl-2,3-(2,3-dimethoxybut-2,3-diyl)-α-D-xylopyranoside (1032939-16-4) + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → 1-O-benzyl-2,3-(2,3-dimethoxybut-2,3-diyl)-α-D-xylopyranoside-4-O-dibenzylphosphate (1032939-17-5)

Conditions	Yield
Stage #1: 1-O-benzyl-2,3-(2,3-dimethoxybut-2,3-diyl)-α-D-xylopyranoside With potassium tert-butylate In tetrahydrofuran at 20℃; for 0.333333h; Inert atmosphere; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at -40 - 20℃; for 3.33333h;	100%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + benzyl 2,3-O-[(2R,3R)-2,3-dimethoxybutane-2,3-dioxy]-β-L-arabinopyranoside (550346-02-6) → 1-O-benzyl-2,3-(2,3-dimethoxybut-2,3-diyl)-β-L-arabinopyranoside-4-O-dibenzylphosphate (1032939-14-2)

Conditions	Yield
Stage #1: benzyl 2,3-O-[(2R,3R)-2,3-dimethoxybutane-2,3-dioxy]-β-L-arabinopyranoside With potassium tert-butylate In tetrahydrofuran at 20℃; for 0.333333h; Inert atmosphere; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at -40 - 20℃; for 3.33333h;	100%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + Glycerinaldehyd-diethylacetal-3-triphenylmethylether (81429-51-8) → 2-dibenzylphosphoryl-3-triphenylmethylglyceraldehyde diethyl acetal (1032939-18-6)

Conditions	Yield
Stage #1: Glycerinaldehyd-diethylacetal-3-triphenylmethylether With potassium tert-butylate In tetrahydrofuran at 20℃; for 0.333333h; Inert atmosphere; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at -40 - 20℃;	99%

methanol-CH2Cl2 + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 4-hydroxy-benzaldehyde (123-08-0) → dibenzyl (4-formylphenyl) phosphate (156745-33-4)

Conditions	Yield
With potassium tert-butylate In tetrahydrofuran	98%

2-acetamido-3-O-acetyl-2-deoxy-4,6-O-(di-tert-butylsilandiyl)-D-glucopyranose + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → C32H46NO10PSi (1092110-69-4)

Conditions	Yield
Stage #1: 2-acetamido-3-O-acetyl-2-deoxy-4,6-O-(di-tert-butylsilandiyl)-D-glucopyranose With lithium diisopropyl amide In tetrahydrofuran at -78℃; for 0.0833333h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at -78 - 20℃; stereoselective reaction;	98%

3-(4-hydroxyphenyl)propan-1-ol (10210-17-0) + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → 3-[4-(dibenzyl)phosphoryloxy]phenyl-1-propanol

Conditions	Yield
With tetrahexylammonium iodide; silver(l) oxide In dichloromethane at 20℃; for 20h;	97%

4-phenyl-butan-1-ol (3360-41-6) + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → 4-phenylbutyl-dibenzylphosphate (136025-58-6)

Conditions	Yield
With titanium(IV) tetrabutoxide; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 16h; Inert atmosphere;	97%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + (1,1-bis-(hydroxymethyl)propyl)carbamic acid benzyl ester (1346041-88-0) → 2-(benzyloxycarbonyl)amino-2-ethyl-3-hydroxylpropyl dibenzyl phosphate

Conditions	Yield
With titanium(IV) tetrabutoxide; N-ethyl-N,N-diisopropylamine In toluene at 20℃; for 16h; Time; Inert atmosphere; chemoselective reaction;	97%
With titanium(IV) tetrabutoxide; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 16h; Solvent; Inert atmosphere;	96%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → dibenzyl (4-formylphenyl) phosphate (156745-33-4)

Conditions	Yield
Stage #1: 4-hydroxy-benzaldehyde With potassium tert-butylate In tetrahydrofuran at 20℃; for 0.166667h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at 70℃; for 1.16667h;	96%

1-O-benzyl-2,3-isopropylidene-β-L-ribopyranose (1032939-22-2) + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → 1-O-benzyl-2,3-isopropylidene-β-L-ribopyranoside-4-O-dibenzylphosphate (1032939-23-3)

Conditions	Yield
Stage #1: 1-O-benzyl-2,3-isopropylidene-β-L-ribopyranose With potassium tert-butylate In tetrahydrofuran at 20℃; for 0.333333h; Inert atmosphere; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at -40 - 20℃; for 5.66667h;	96%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + (S)-1-(3,4,5-trimethoxyphenyl)-4-(3-hydroxy-4-methoxyphenyl)-3-methyleneazetidine-2-one → C34H34NO9P

Conditions	Yield
With sodium hydride In dichloromethane at 0 - 20℃; for 0.25h; Schlenk technique;	96%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + (1S,2S,3R,4S,5S,6R)-3-Benzyloxy-5-(1-ethoxy-ethoxy)-6-fluoro-cyclohexane-1,2,4-triol (129365-65-7) → Phosphoric acid dibenzyl ester (1S,2S,3R,4S,5S,6S)-2-benzyloxy-3,4-bis-(bis-benzyloxy-phosphoryloxy)-6-(1-ethoxy-ethoxy)-5-fluoro-cyclohexyl ester (129365-66-8)

Conditions	Yield
With sodium hydride In N,N-dimethyl-formamide at 0℃; for 8h;	95%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 2,3,4,6-tetra-O-benzyl-D-mannopyranose (4132-28-9, 4291-69-4, 6386-24-9, 6564-72-3, 59531-24-7, 69257-52-9, 78184-89-1, 78609-16-2, 78609-17-3, 78609-18-4, 96553-53-6, 104111-61-7, 131347-08-5) → dibenzyl 2,3,4,6-tetra-O-benzyl-α-D-mannopyranosyl phosphate (90357-98-5)

Conditions	Yield
With lithium diisopropyl amide In tetrahydrofuran; hexane; ethylbenzene at -78℃; for 3h;	95%

N6-methyl-2-(2-phenylethynyl)-2'-deoxyadenosine (691409-52-6) + dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) → N6-methyl-2-(2-phenylethynyl)-2'-deoxyadenosine-3',5'-bis(dibenzylphosphate) (691409-55-9)

Conditions	Yield
Stage #1: N6-methyl-2-(2-phenylethynyl)-2'-deoxyadenosine With potassium tert-butylate In tetrahydrofuran at -40℃; for 0.0833333h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at -40℃; for 0.5h;	95%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 2-(3-fluorophenyl)-5-hydroxy-6-methoxyquinolin-4-one (1256037-41-8) → 2-(3-fluorophenyl)-6-methoxyquinoline-4,5-diyl bis(dibenzylphosphate) (1256037-56-5)

Conditions	Yield
Stage #1: 2-(3-fluorophenyl)-5-hydroxy-6-methoxyquinolin-4-one With sodium hydride In tetrahydrofuran at 0℃; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran for 0.416667h;	95%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 2-azido-4,6-di-O-benzyl-2,3-dideoxy-3-fluoro-α/β-D-glucopyranose → (2-azido-4,6-di-O-benzyl-2,3-dideoxy-3-fluoro-α-D-glucopyranosyl)-1-dibenzylphosphate (1334530-12-9)

Conditions	Yield
Stage #1: 2-azido-4,6-di-O-benzyl-2,3-dideoxy-3-fluoro-α/β-D-glucopyranose With ethylbenzene; lithium diisopropyl amide In tetrahydrofuran; n-heptane at -78℃; for 0.25h; Inert atmosphere; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran; n-heptane at -78 - 0℃; for 3h; Inert atmosphere;	95%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 2-(3-fluorophenyl)-5-hydroxy-6-methoxyquinolin-4-one (1256037-41-8) → 2-(3-fluorophenyl)-6-methoxyquinoline-4,5-diyl bis(dibenzylphosphate) (1256037-56-5)

Conditions	Yield
Stage #1: 2-(3-fluorophenyl)-5-hydroxy-6-methoxyquinolin-4-one With sodium hydride In tetrahydrofuran at -1 - 1℃; for 1h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran for 0.416667h; Product distribution / selectivity;	95%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 1,5-anhydro-3,4-di-O-benzyl-2-deoxy-5a-carba-D-arabino-hex-1-enitol (207564-31-6) → C35H37O6P

Conditions	Yield
With sodium hydride In N,N-dimethyl-formamide at 0 - 20℃;	95%

dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate (990-91-0) + 2-chloro-9-[(diethanolamino)carboxymethyl]-6-methylamino-purine (262863-48-9) → 9-bis(2-dibenzylphosphatoethylamino)-acetyl-2-chloro-6-methylamino-purine (262863-49-0)

Conditions	Yield
Stage #1: 2-chloro-9-[(diethanolamino)carboxymethyl]-6-methylamino-purine With lithium diisopropyl amide In tetrahydrofuran at -78℃; for 0.25h; deprotonation; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In tetrahydrofuran at 0 - 25℃; for 12h; phosphorylation; Further stages.;	94%

Upstream product

• 110-86-1 pyridine 
• 1623-08-1 phosphoric acid dibenzyl ester 
• 98-59-9 p-toluenesulfonyl chloride 
• 71-43-2 benzene 
• 98-74-8 4-Nitrobenzenesulfonyl chloride 
• 100-51-6 benzyl alcohol 
• 91-66-7 N,N-diethylaniline 
• 18826-95-4 1.3-butanediol 
• 15205-57-9 tribenzyl phosphite 
• 538-37-4 dibenzyl phosphochloridate 
• 75-62-7 Bromotrichloromethane 
• 17176-77-1 Dibenzyl phosphite 
• 56-23-5 tetrachloromethane 
• 121-44-8 triethylamine 

Downstream Products

• 102660-99-1 phenylcarbamimidoyl-amidophosphoric acid dibenzyl ester 
• 122351-24-0 benzyl 2-acetamido-3,6-di-O-benzyl-2-deoxy-β-D-glucopyranoside 4-(dibenzyl phosphate) 
• 115432-19-4 Phosphoric acid dibenzyl ester (1S,2R,3S,4S,5R,6R)-2,3,4,5-tetrakis-benzyloxy-6-(bis-benzyloxy-phosphoryloxy)-cyclohexyl ester 
• 148888-53-3 1D-2,3,6-trideoxy-myo-inositol 1,4,5-tris(dibenzylphosphate) 
• 115432-21-8 Acetic acid (1R,2S,3S,4R,5S,6R)-2,3,4-triacetoxy-5,6-bis-(bis-benzyloxy-phosphoryloxy)-cyclohexyl ester 
• 141843-90-5 (E)-3-[4-(Bis-benzyloxy-phosphoryloxy)-3-methoxy-phenyl]-acrylic acid methyl ester 
• 115457-82-4 C₆₈H₇₂O₁₈P₄ 
• 115510-56-0 C₅₄H₅₈O₁₂P₂ 
• 129801-84-9 Phosphoric acid dibenzyl ester (1R,2R,4R)-2,4-bis-benzyloxy-cyclohexyl ester 
• 115510-57-1 D-1,3,6-tri-O-benzyl-2,4,5-tris-O-[di(benzyloxy)phosphoryl]-myo-inositol 
• 116907-55-2 1L-1,2,4-tri-O-benzyl-3,5,6-tris-O-dibenzyloxyphosphoryl-myo-inositol 
• 114342-70-0 Phosphoric acid dibenzyl ester (1R,2R,3R,4R,5R,6S)-2,3,6-tris-benzyloxy-4,5-bis-(bis-benzyloxy-phosphoryloxy)-cyclohexyl ester 
• 125291-05-6 (3aα,4α,5β,7β,7aα)-hexahydro-2,2-dimethylbenzo-1,3(2H)-dioxol-4,5,7-triol tris(dibenzylphosphate) 
• 125291-11-4 (3aα,4α,5β,6α,7β,7aα)-hexahydro-2,2,6-trimethylbenzo-1,3(2H)-dioxol-4,5,7-triol tris(dibenzylphosphate) 

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