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35180-01-9 Usage

Chemical Properties

Clear Colourless Liquid

Check Digit Verification of cas no

The CAS Registry Mumber 35180-01-9 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,5,1,8 and 0 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 35180-01:
(7*3)+(6*5)+(5*1)+(4*8)+(3*0)+(2*0)+(1*1)=89
89 % 10 = 9
So 35180-01-9 is a valid CAS Registry Number.
InChI:InChI=1/C5H9ClO3/c1-4(2)9-5(7)8-3-6/h4H,3H2,1-2H3

35180-01-9 Well-known Company Product Price

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  • USP

  • (1115705)  Chloromethyl isopropyl carbonate  United States Pharmacopeia (USP) Reference Standard

  • 35180-01-9

  • 1115705-100MG

  • 14,500.98CNY

  • Detail

35180-01-9SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 11, 2017

Revision Date: Aug 11, 2017

1.Identification

1.1 GHS Product identifier

Product name Chloromethyl isopropyl carbonate

1.2 Other means of identification

Product number -
Other names isopropyloxycarbonyloxymethyl chloride

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:35180-01-9 SDS

35180-01-9Synthetic route

carbonochloridic acid, chloromethyl ester
22128-62-7

carbonochloridic acid, chloromethyl ester

isopropyl alcohol
67-63-0

isopropyl alcohol

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

Conditions
ConditionsYield
With triethylamine at 0℃;98%
With pyridine In diethyl ether; isopropyl alcohol at 10℃; for 18h; Cooling;95%
With pyridine In diethyl ether at 0 - 20℃;92%
formaldehyd
50-00-0

formaldehyd

isopropyl chloroformate
108-23-6

isopropyl chloroformate

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

Conditions
ConditionsYield
With 1-ethyl-3-methylimidazolium tetrafluoroborate In toluene at 10℃; Reagent/catalyst; Solvent; Temperature;95%
chloromethyl formate
30566-31-5

chloromethyl formate

isopropyl alcohol
67-63-0

isopropyl alcohol

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

isopropyloxycarbonyloxymethyl iodide
258841-42-8

isopropyloxycarbonyloxymethyl iodide

Conditions
ConditionsYield
With sodium iodide In acetonitrile at 60℃; for 3h;99%
With sodium hydrogencarbonate; sodium iodide In acetone92%
With sodium iodide In acetonitrile at 30℃; for 22h; Inert atmosphere;91.5%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

(3S)-1-[(2R)-2-[4-(2-chloro-4-fluorophenyl)-2-oxochromen-7-yl]oxypropanoyl]piperidine-3-carboxylic acid

(3S)-1-[(2R)-2-[4-(2-chloro-4-fluorophenyl)-2-oxochromen-7-yl]oxypropanoyl]piperidine-3-carboxylic acid

isopropoxycarbonyloxymethyl (3S)-1-[(2R)-2-[4-(2-chloro-4-fluorophenyl)-2-oxochromen-7-yl]oxypropanoyl]piperidine-3-carboxylate

isopropoxycarbonyloxymethyl (3S)-1-[(2R)-2-[4-(2-chloro-4-fluorophenyl)-2-oxochromen-7-yl]oxypropanoyl]piperidine-3-carboxylate

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl-formamide at 50℃; for 0.5h;93%
3-[[3-ethyl-1,2,3,6-tetrahydro-5-(1-methylethyl)-2,6-dioxo-4-pyrimidinyl]carbonyl]-5-methylbenzonitrile
1097628-00-6

3-[[3-ethyl-1,2,3,6-tetrahydro-5-(1-methylethyl)-2,6-dioxo-4-pyrimidinyl]carbonyl]-5-methylbenzonitrile

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

C23H27N3O6
1099828-46-2

C23H27N3O6

Conditions
ConditionsYield
With sodium hydride In N,N-dimethyl-formamide92%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

tenofovir
147127-20-6

tenofovir

tenofovir disoproxil

tenofovir disoproxil

Conditions
ConditionsYield
With tetrabutylammomium bromide; triethylamine In 1-methyl-pyrrolidin-2-one at 50℃; Temperature;91.5%
With triethylamine; N-butylpyridinium tetrafluoroborate at 40℃; for 1.5h; Reagent/catalyst; Temperature;90.6%
Stage #1: tenofovir With tetrabutylammomium bromide; triethylamine In 1-methyl-pyrrolidin-2-one at 50℃; for 0.5h;
Stage #2: chloromethyl isopropyl carbonate In 1-methyl-pyrrolidin-2-one at 60℃; for 4h; Reagent/catalyst; Solvent;
87.6%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

1-[3-[allyl(methoxy)phosphoryl]oxypropoxy]hexadecane
1258789-65-9

1-[3-[allyl(methoxy)phosphoryl]oxypropoxy]hexadecane

HDP-POC allylphosphonate
1258789-66-0

HDP-POC allylphosphonate

Conditions
ConditionsYield
With sodium iodide In acetonitrile for 72h; Reflux; Inert atmosphere;91%
With sodium iodide In acetonitrile for 72h; Reflux; Inert atmosphere;
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

(2E)-but-2-enedioic acid
110-17-8

(2E)-but-2-enedioic acid

tenofovir
147127-20-6

tenofovir

tenofovir disoproxyl fumarate
202138-50-9

tenofovir disoproxyl fumarate

Conditions
ConditionsYield
Stage #1: tenofovir With triethylamine In 1-methyl-pyrrolidin-2-one at 63℃; for 0.5h;
Stage #2: chloromethyl isopropyl carbonate In 1-methyl-pyrrolidin-2-one at 63℃; for 4h;
Stage #3: (2E)-but-2-enedioic acid In isopropyl alcohol at 50℃; for 0.5h; Concentration;
90%
Stage #1: chloromethyl isopropyl carbonate; tenofovir With tetrabutylammomium bromide; triethylamine at 50℃; for 3h; Inert atmosphere;
Stage #2: (2E)-but-2-enedioic acid In isopropyl alcohol Reagent/catalyst; Temperature; Reflux;
78.8%
Stage #1: chloromethyl isopropyl carbonate; tenofovir With tetrabutylammomium bromide; triethylamine In 1-methyl-pyrrolidin-2-one; toluene at 45 - 55℃; for 5h;
Stage #2: (2E)-but-2-enedioic acid In isopropyl alcohol at 50 - 55℃; for 2h;
63.6%
R-361015

R-361015

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

C21H26ClNO7S

C21H26ClNO7S

Conditions
ConditionsYield
With thionyl chloride at 80℃; for 4h;87%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

benzylamine
100-46-9

benzylamine

isopropyl N-benzylcarbamate
5338-49-8

isopropyl N-benzylcarbamate

Conditions
ConditionsYield
In benzene a.) RT, 1 h, b.) reflux, 1 h;85.4%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

C16H28N5O7P

C16H28N5O7P

C26H44N5O13P

C26H44N5O13P

Conditions
ConditionsYield
With triethylamine In 1-methyl-pyrrolidin-2-one; ethanol at 20 - 55℃; for 6h;85.4%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

1-[(2'-t-butoxycarbonylbiphenyl-4-yl)methyl]-4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylic acid
144690-41-5

1-[(2'-t-butoxycarbonylbiphenyl-4-yl)methyl]-4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylic acid

isopropoxycarbonyloxymethyl 1-[(2'-t-butoxycarbonylbiphenyl-4-yl)methyl]-4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5carboxylate
144690-43-7

isopropoxycarbonyloxymethyl 1-[(2'-t-butoxycarbonylbiphenyl-4-yl)methyl]-4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5carboxylate

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl acetamide at 20 - 50℃; for 3h;85%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

5-((4'-isopropyl-[1,1'-biphenyl]-4-yl)oxy)-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylic acid

5-((4'-isopropyl-[1,1'-biphenyl]-4-yl)oxy)-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylic acid

((isopropoxycarbonyl)oxy)methyl 5-((4'-isopropyl-[1,1'-biphenyl]-4-yl)oxy)-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylate

((isopropoxycarbonyl)oxy)methyl 5-((4'-isopropyl-[1,1'-biphenyl]-4-yl)oxy)-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylate

Conditions
ConditionsYield
Stage #1: 5-((4'-isopropyl-[1,1'-biphenyl]-4-yl)oxy)-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylic acid With potassium carbonate In N,N-dimethyl acetamide at 20℃; for 0.5h;
Stage #2: chloromethyl isopropyl carbonate In N,N-dimethyl acetamide at 50℃; for 6h;
84.1%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

5-(3-methylbut-1-ynyl)-3-[(trans-4-methylcyclohexanecarbonyl)-[(1S)-1-(morpholine-4-carbonyl)propyl]amino]thiophene-2-carboxylic acid.

5-(3-methylbut-1-ynyl)-3-[(trans-4-methylcyclohexanecarbonyl)-[(1S)-1-(morpholine-4-carbonyl)propyl]amino]thiophene-2-carboxylic acid.

C32H46N2O8S

C32H46N2O8S

Conditions
ConditionsYield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.333333h; Microwave irradiation;83%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

3-[[(1S)-1-(dimethylcarbamoyl)propyl]-(trans-4-methylcyclohexanecarbonyl)amino]-5-(3-methylbut-1-ynyl)thiophene-2-carboxylic acid

3-[[(1S)-1-(dimethylcarbamoyl)propyl]-(trans-4-methylcyclohexanecarbonyl)amino]-5-(3-methylbut-1-ynyl)thiophene-2-carboxylic acid

C31H46N2O6S

C31H46N2O6S

Conditions
ConditionsYield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.333333h; Microwave irradiation;80%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

N-(3-(3,6-difluoropyridin-2-yl)-1-((1r,4r)-4-ethoxycyclohexyl)-1H-pyrazol-4-yl)-2-(1H-pyrazol-4-yl)thiazole-4-carboxamide

N-(3-(3,6-difluoropyridin-2-yl)-1-((1r,4r)-4-ethoxycyclohexyl)-1H-pyrazol-4-yl)-2-(1H-pyrazol-4-yl)thiazole-4-carboxamide

(4-(4-((3-(3,6-difluoropyridin-2-yl)-1-((1r,4r)-4-ethoxycyclohexyl)-1H-pyrazol-4-yl)carbamoyl)thiazol-2-yl)-1H-pyrazol-1-yl)methyl isopropyl carbonate

(4-(4-((3-(3,6-difluoropyridin-2-yl)-1-((1r,4r)-4-ethoxycyclohexyl)-1H-pyrazol-4-yl)carbamoyl)thiazol-2-yl)-1H-pyrazol-1-yl)methyl isopropyl carbonate

Conditions
ConditionsYield
With caesium carbonate In N,N-dimethyl-formamide at 20℃;80%
With caesium carbonate In N,N-dimethyl-formamide at 20℃;80%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

5-(3,3-dimethylbut-1-ynyl)-3-[(trans-4-methylcyclohexanecarbonyl)-(2-oxo-2-thiomorpholino-ethyl)amino]thiophene-2-carboxylic acid

5-(3,3-dimethylbut-1-ynyl)-3-[(trans-4-methylcyclohexanecarbonyl)-(2-oxo-2-thiomorpholino-ethyl)amino]thiophene-2-carboxylic acid

C30H42N2O8S

C30H42N2O8S

Conditions
ConditionsYield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.333333h; Microwave irradiation;76%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

(1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-[(3,4-dichlorobenzyl)oxy]-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid
1377990-58-3

(1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-[(3,4-dichlorobenzyl)oxy]-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid

bis({[(1-methylethoxy)carbonyl]oxy}methyl) (1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-[(3,4-dichlorobenzyl)oxy]-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylate
1377990-61-8

bis({[(1-methylethoxy)carbonyl]oxy}methyl) (1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-[(3,4-dichlorobenzyl)oxy]-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylate

Conditions
ConditionsYield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide for 18h; Product distribution / selectivity;76%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

tenofovir
147127-20-6

tenofovir

Tenofovir mono-POC

Tenofovir mono-POC

Conditions
ConditionsYield
With triethylamine In N,N-dimethyl-formamide at 20 - 40℃; for 12h; Temperature;76%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

C12H20N5O4P

C12H20N5O4P

propan-2-yl {[(propan-2-yloxy)carbonyl]oxy}methyl {[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methanephosphonate

propan-2-yl {[(propan-2-yloxy)carbonyl]oxy}methyl {[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methanephosphonate

Conditions
ConditionsYield
With triethylamine In N,N-dimethyl-formamide at 45 - 50℃; for 1h;75.6%
allylphosphonic acid dimethyl ester
757-54-0

allylphosphonic acid dimethyl ester

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

bis-POC-allylphosphonate
1258789-64-8

bis-POC-allylphosphonate

Conditions
ConditionsYield
With sodium iodide In acetonitrile for 72h; Inert atmosphere; Reflux;75%
With sodium iodide In acetonitrile for 48h; Reflux; Inert atmosphere;5.75 g
formic acid
64-18-6

formic acid

4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3’,4’:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone
313368-91-1

4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3’,4’:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

(6bR,10aS)-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-8-isopropoxycarbonyloxymethyl-3-methyl-2,3,6b,7,8,9,10,10a-octahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8-ium formate

(6bR,10aS)-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-8-isopropoxycarbonyloxymethyl-3-methyl-2,3,6b,7,8,9,10,10a-octahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8-ium formate

Conditions
ConditionsYield
Stage #1: 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3’,4’:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone; chloromethyl isopropyl carbonate With sodium iodide In acetonitrile at 20℃; for 168h;
Stage #2: formic acid In water; acetonitrile for 0.366667h;
75%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

{[(4-methylbenzenesulfonyl)oxy]methyl}phosphonic acid
161760-09-4

{[(4-methylbenzenesulfonyl)oxy]methyl}phosphonic acid

C18H27O12PS

C18H27O12PS

Conditions
ConditionsYield
Stage #1: tosyloxymethylphosphonic acid monoethyl ester With triethylamine In N,N-dimethyl-formamide at 20℃; for 1h;
Stage #2: chloromethyl isopropyl carbonate In N,N-dimethyl-d6-formamide at 60℃; for 5h; Solvent; Reagent/catalyst;
75%
3-tert-Butyl-4-hydroxyanisole
121-00-6

3-tert-Butyl-4-hydroxyanisole

chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

(2-tert-butyl-4-methoxyphenoxy)methyl carbonate isopropyl ester

(2-tert-butyl-4-methoxyphenoxy)methyl carbonate isopropyl ester

Conditions
ConditionsYield
Stage #1: 3-tert-Butyl-4-hydroxyanisole With sodium hydride In tetrahydrofuran for 0.5h;
Stage #2: chloromethyl isopropyl carbonate In tetrahydrofuran at 20℃; for 24h;
75%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

C17H25O7P

C17H25O7P

5-benzyl 1-(((isopropoxycarbonyl)oxy)methyl) 2-((diethoxyphosphoryl)methyl)pentanedioate

5-benzyl 1-(((isopropoxycarbonyl)oxy)methyl) 2-((diethoxyphosphoryl)methyl)pentanedioate

Conditions
ConditionsYield
Stage #1: C17H25O7P With potassium carbonate; sodium iodide In acetonitrile at 20℃; for 0.25h;
Stage #2: chloromethyl isopropyl carbonate In acetonitrile at 50℃;
72%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1H)-one
1354745-52-0

6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1H)-one

ELQ-330

ELQ-330

Conditions
ConditionsYield
With tetra-(n-butyl)ammonium iodide; potassium carbonate In N,N-dimethyl-formamide at 60℃; for 2h; Inert atmosphere;72%
With tetra-(n-butyl)ammonium iodide; potassium carbonate In N,N-dimethyl-formamide at 60℃;
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

C12H11ClN2O2

C12H11ClN2O2

C17H19ClN2O5

C17H19ClN2O5

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 3h;70.5%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

5-(3,3-dimethylbut-1-yn-1-yl)-3-(4-methyl-N-((S)-1-methyl-2-oxoazepan-3-yl)cyclohexanecarboxamido)thiophene-2-carboxylic acid

5-(3,3-dimethylbut-1-yn-1-yl)-3-(4-methyl-N-((S)-1-methyl-2-oxoazepan-3-yl)cyclohexanecarboxamido)thiophene-2-carboxylic acid

C31H44N2O7S

C31H44N2O7S

Conditions
ConditionsYield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.5h; Microwave irradiation;70%
chloromethyl isopropyl carbonate
35180-01-9

chloromethyl isopropyl carbonate

(1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-{[(3,4-difluorophenyl)sulfanyl]methyl}-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid
1377615-94-5

(1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-{[(3,4-difluorophenyl)sulfanyl]methyl}-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid

bis({[(1-methylethoxy)carbonyl]oxy}methyl) (1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-{[(3,4-difluorophenyl)sulfanyl]methyl}-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylate
1377616-01-7

bis({[(1-methylethoxy)carbonyl]oxy}methyl) (1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-{[(3,4-difluorophenyl)sulfanyl]methyl}-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylate

Conditions
ConditionsYield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 25℃; for 12h; Product distribution / selectivity; Inert atmosphere;70%

35180-01-9Relevant articles and documents

The shortest strategy for generating phosphonate prodrugs by olefin cross-metathesis - Application to acyclonucleoside phosphonates

Pradere, Ugo,Clavier, Herve,Roy, Vincent,Nolan, Steven P.,Agrofoglio, Luigi A.

, p. 7324 - 7330 (2011)

A short synthetic route to phosphonate prodrugs by olefin cross-metathesis, which uses either (acyloxymethyl) or (hexadecyloxypropyl) allylphosphonate building blocks is described. A study of eight ruthenium catalysts including the Ru-indenylidene catalyst, which bears the N-heterocyclic carbene 1,3-bis(2,6-diisopropylphenyl)-4,5-dihydroimidazol-2-ylidene, was undertaken. This method was applied to the synthesis of acyclonucleoside phosphonate prodrugs. This strategy is appealing for further uses in pharmaceutical and medicinal research. A short synthetic route to phosphonate prodrugs by olefin cross-metathesis, which uses either (acyloxymethyl)- or (hexadecyloxypropyl) allylphosphonate building blocks, is described. A study of eight Ru catalysts including the Ru-indenylidene catalyst, which bears an N-heterocycliccarbene, was undertaken. This method was applied to the synthesis of acyclonucleoside phosphonate prodrugs. Copyright

Benzodiazepine compound as well as preparation method and medical action thereof (by machine translation)

-

Paragraph 0204-0206; 0310; 0311; 0313, (2021/01/11)

The invention provides a benzodiazepine compound as well as a preparation method and a medicine effect thereof, and belongs to the field of chemical medicine. The benzodiazepine compound is a compound shown in formula I. Or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a eutectic thereof, or a composition thereof. The anesthetic effect of the compound of the invention is good, and the anesthetic effect of the compound is equivalent to that of Ramozolam, and even better than that of repirzolam, and particularly shows that the effective dosage is obviously reduced, and the duration and the recovery time are remarkably reduced. At the same time, in the rat tail vein anesthesia model, the compound of the present invention is remarkably improved in comparison with the quality of the Ramozolam wake-up. The compound has the advantages of high effectiveness, short duration, fast resuscitation and good tolerance, can be used for anesthesia induction, anesthesia maintenance and inter-day operation anesthesia, and has a good application prospect. (by machine translation)

N-substituted imidazole carboxylate compound, preparation method and use thereof

-

Paragraph 0025, (2018/03/26)

A N-substituted imidazole carboxylate compound shown as a formula (I), a preparation method and use thereof are disclosed. In the formula (I), C * is a R type chiral carbon atom, R 1 and R 2 are independently selected from the group consisting of H, methyl, ethyl, cyclopropyl, cyclobutyl or isopropyl or a C2-5 ene-group formed by R1 and R2; and R3 is substituted or unsubstituted C1-18 saturated orunsaturated aliphatic hydrocarbon or aromatic hydrocarbon, wherein the aliphatic hydrocarbon includes a linear, branched or cyclic aliphatic hydrocarbon group. The N-substituted imidazole carboxylatecompound or pharmaceutically acceptable salts thereof can be used to prepare central inhibitory drugs that exert sedative, hypnotic and/or anesthetic effects on humans or animals, can produce rapid and reversible anesthetic effects, and rapidly metabolises into inactive etomidate acid, and after drug withdrawal, recovery quality is good; body's corticosteroid function can be quickly recovered after single administration or continuous administration, the incidence of muscle tremor is low after the administration, and after the drug withdrawal, the recovery is quick.

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