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138786-67-1

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138786-67-1 Usage

Chemical Properties

White to Off-White Solid

Originator

Controloc,Byk Gulden ,Germany

Uses

Different sources of media describe the Uses of 138786-67-1 differently. You can refer to the following data:
1. An antiulcerative. Gastric pump inhibitor.
2. An antiulcerative. Gastric pump inhibitor
3. Gastrointestinal

Brand name

Protonix (Wyeth).

Therapeutic Function

Antiulcer

General Description

Pantoprazole sodium, racemicsodium5-(difluoromethoxy)-2-[[3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sesquihydrate is a white tooff-white crystalline powder that is freely soluble in water,very slightly soluble in phosphate buffer at pH 7.4, and practicallyinsoluble in n-hexane. The benzimidazole of this drughas a weakly basic nitrogen (pyridine N, pKa 3.83) and an benzimidazoleproton (pKa 0.11), facilitating formulation as asodium salt. The stability of the compound in aqueous solutionis pH dependent; the rate of degradation increases with decreasingpH. At ambient temperature, the degradation half-lifeis approximately 2.8 hours at pH 5.0 and approximately 220hours at pH 7.8.The absorption of pantoprazole is rapid (Cmax of2.5μg/mL, Tmax 2.5 hours) after single or multiple oral40-mg doses. Pantoprazole is well absorbed (77% bioavailability).Administration with food may delay its absorptionbut does not alter pantoprazole bioavailability. Pantoprazoleis distributed mainly in extracellular fluid. The serum proteinbinding of pantoprazole is about 98%, primarily to albumin.Pantoprazole is extensively metabolized in the liver throughthe CYP system, including O-demethylation (CYP2C19),with subsequent sulfation. Other metabolic pathways includesulfur oxidation by CYP3A4. There is no evidencethat any of the pantoprazole metabolites have significantpharmacological activity. Approximately 71% of a dose of pantoprazole is excreted in the urine, with 18% excretedin the feces through biliary excretion.

Check Digit Verification of cas no

The CAS Registry Mumber 138786-67-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,8,7,8 and 6 respectively; the second part has 2 digits, 6 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 138786-67:
(8*1)+(7*3)+(6*8)+(5*7)+(4*8)+(3*6)+(2*6)+(1*7)=181
181 % 10 = 1
So 138786-67-1 is a valid CAS Registry Number.
InChI:InChI=1/C16H14F2N3O4S.Na/c1-23-13-5-6-19-12(14(13)24-2)8-26(22)16-20-10-4-3-9(25-15(17)18)7-11(10)21-16;/h3-7,15H,8H2,1-2H3;/q-1;+1/rC16H14F2N3NaO4S/c1-24-13-5-6-19-11(14(13)25-2)8-27(23)16-20-10-7-9(26-15(17)18)3-4-12(10)21(16)22/h3-7,15H,8H2,1-2H3

138786-67-1 Well-known Company Product Price

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  • Sigma-Aldrich

  • (Y0001001)  Pantoprazole for system suitability  European Pharmacopoeia (EP) Reference Standard

  • 138786-67-1

  • Y0001001

  • 1,880.19CNY

  • Detail

138786-67-1SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name pantoprazole sodium

1.2 Other means of identification

Product number -
Other names Pantoprazole Sodium Salt

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:138786-67-1 SDS

138786-67-1Synthetic route

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole
102625-70-7

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
With sodium hydroxide In water; acetonitrile at 20℃;95%
With sodium hydroxide In ethanol for 5h; Reflux;95%
With sodium hydroxide In water; ethyl acetate at 20℃; for 5.5h;92%
pantoprazole sulfide
102625-64-9

pantoprazole sulfide

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
Stage #1: pantoprazole sulfide With sodium hydroxide; tert-butylhypochlorite In dichloromethane; water at 0 - 5℃; for 1h;
Stage #2: With sodium hydroxide In water; acetone at 0 - 25℃; for 7h;
95%
Stage #1: pantoprazole sulfide With potassium tungstate dihydrate; dihydrogen peroxide at -5 - 0℃; for 4.5h; pH=3.5;
Stage #2: With sodium hydroxide In water at 20℃; Temperature; Reagent/catalyst;
78.7%
With sodium hypochlorite; sodium hydroxide In methanol; water at -20 - -5℃;
Stage #1: pantoprazole sulfide With sodium hypochlorite; sodium hydroxide In water; acetonitrile at -5 - 30℃;
Stage #2: With acetic acid In dichloromethane at 25 - 30℃; pH=8 - 8.5;
Stage #3: With sodium hydroxide In dichloromethane; water at 25 - 30℃; Concentration;
Stage #1: pantoprazole sulfide With sodium hypochlorite; water; sodium hydroxide In ethyl acetate at 0 - 10℃; for 7h;
Stage #2: With sodium thiosulfate In ethyl acetate for 0.333333h;
5-(difluoromethoxy)-2-mercapto-1H-benzimidazole
97963-62-7

5-(difluoromethoxy)-2-mercapto-1H-benzimidazole

2-Chloromethyl-3,4-dimethoxy-pyridine; hydrochloride
72830-09-2

2-Chloromethyl-3,4-dimethoxy-pyridine; hydrochloride

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
Stage #1: 5-(difluoromethoxy)-2-mercapto-1H-benzimidazole; 2-Chloromethyl-3,4-dimethoxy-pyridine; hydrochloride With sodium hydroxide; tetrabutylammomium bromide In dichloromethane; water at 25 - 30℃; for 12h;
Stage #2: With sodium hydroxide; sodium hypochlorite In dichloromethane; water at 0 - 8℃; for 6h; Product distribution / selectivity;
83%
2-hydroxymethyl-3,4-dimethoxypyridine hydrochloride

2-hydroxymethyl-3,4-dimethoxypyridine hydrochloride

5-(difluoromethoxy)-2-mercapto-1H-benzimidazole
97963-62-7

5-(difluoromethoxy)-2-mercapto-1H-benzimidazole

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
Stage #1: 2-hydroxymethyl-3,4-dimethoxypyridine hydrochloride With thionyl chloride In dichloromethane at 0 - 15℃; for 1h;
Stage #2: 5-(difluoromethoxy)-2-mercapto-1H-benzimidazole With sodium hydroxide; tetrabutylammomium bromide In dichloromethane; water at 10 - 30℃; for 12h; pH=10 - 11;
Stage #3: With sodium hydroxide; sodium hypochlorite In dichloromethane; water at 0 - 8℃; for 6h; Product distribution / selectivity;
79.6%
(5-difluoromethoxy)-2-[(4-chloro-3-methoxy-2-pyridinyl)methyl]thio-1H-benzimidazole
368890-20-4

(5-difluoromethoxy)-2-[(4-chloro-3-methoxy-2-pyridinyl)methyl]thio-1H-benzimidazole

sodium methylate
124-41-4

sodium methylate

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
In methanol at 50℃; Heating / reflux;70.8%
5-(difluoromethoxy)-2-[[(4-chloro-3-methoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole
409098-86-8

5-(difluoromethoxy)-2-[[(4-chloro-3-methoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
With sodium methylate In methanol at 50℃; Heating / reflux;70.8%
pantoprazole sulfide
102625-64-9

pantoprazole sulfide

A

5-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl-1-oxide)methylsulfonyl]-1H-benzoimidazole

5-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl-1-oxide)methylsulfonyl]-1H-benzoimidazole

B

pantoprazole sodium
138786-67-1

pantoprazole sodium

C

Pantoprazole sulfone

Pantoprazole sulfone

Conditions
ConditionsYield
With sodium hydroxide; sodium hypochlorite In water; ethyl acetate at -5℃; for 1 - 1.5h; Product distribution / selectivity;A n/a
B 65%
C n/a
5-(difluoromethoxy)-2-mercapto-1H-benzimidazole
97963-62-7

5-(difluoromethoxy)-2-mercapto-1H-benzimidazole

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: sodium hydroxide / ethanol / 8 h / 80 °C
2: 3-chloro-benzenecarboperoxoic acid / chloroform / 4 h / 0 °C
3: sodium hydroxide / ethanol / 5 h / Reflux
View Scheme
Multi-step reaction with 3 steps
1: sodium hydroxide / water; methanol / 3.5 h / 40 - 55 °C
2: LACTIC ACID; peracetic acid / methanol; dichloromethane / 1 h / -25 - -20 °C
3: sodium hydroxide / water; acetone / 40 - 45 °C
View Scheme
sodium hydroxide
1310-73-2

sodium hydroxide

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole
102625-70-7

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
In water; acetonitrile at 25 - 35℃; for 1h;
In ethanol; dichloromethane; water at 20℃; pH=12.5; Product distribution / selectivity;
2-chloromethyl-3,4-dimethoxypyridine hydrochloride

2-chloromethyl-3,4-dimethoxypyridine hydrochloride

5-(difluoromethoxy)-2-mercapto-1H-benzimidazole
97963-62-7

5-(difluoromethoxy)-2-mercapto-1H-benzimidazole

pantoprazole sodium
138786-67-1

pantoprazole sodium

Conditions
ConditionsYield
Stage #1: 2-chloromethyl-3,4-dimethoxypyridine hydrochloride; 5-(difluoromethoxy)-2-mercapto-1H-benzimidazole With sodium hydroxide In ethanol; water at 35℃; for 2h;
Stage #2: With sodium borate In ethanol at 45℃; for 2h;
Stage #3: With dihydrogen peroxide In water at 20℃; for 2.5h; Concentration; Temperature;
19.61 g
pantoprazole sodium
138786-67-1

pantoprazole sodium

zinc (S)-bis{[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)-methylsulphinyl]-1H-benzimidazolide}

zinc (S)-bis{[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)-methylsulphinyl]-1H-benzimidazolide}

Conditions
ConditionsYield
With zinc(II) chloride In water at 20℃; for 1.5h;95%
pantoprazole sodium
138786-67-1

pantoprazole sodium

magnesium {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

magnesium {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

Conditions
ConditionsYield
Stage #1: pantoprazole sodium With sodium hydroxide In water at 25℃; for 1h;
Stage #2: With magnesium chloride In water at 25℃; for 1h;
94.6%
pantoprazole sodium
138786-67-1

pantoprazole sodium

zinc(II) chloride
7646-85-7

zinc(II) chloride

zinc {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

zinc {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

Conditions
ConditionsYield
Stage #1: pantoprazole sodium With sodium hydroxide In water at 25℃; for 1h;
Stage #2: zinc(II) chloride In water at 25℃; for 20h;
94.2%
(S)-1,1,2-triphenyl-1,2-ethanediol
108998-83-0

(S)-1,1,2-triphenyl-1,2-ethanediol

pantoprazole sodium
138786-67-1

pantoprazole sodium

C20H18O2*C16H15F2N3O4S

C20H18O2*C16H15F2N3O4S

Conditions
ConditionsYield
With acetic acid In ethanol for 0.5h; pH=7 - 8; Reflux; Industrial scale;94%
pantoprazole sodium
138786-67-1

pantoprazole sodium

pantoprazole sodium sesquihydrate

pantoprazole sodium sesquihydrate

Conditions
ConditionsYield
With water In tert-butyl methyl ether at 20 - 30℃; for 12h; Product distribution / selectivity;92.4%
With water In di-isopropyl ether at 20 - 30℃; for 1 - 12h; Product distribution / selectivity;91.93%
With water In diethyl ether at 20 - 30℃; for 12h; Product distribution / selectivity;91.93%
With water at 0 - 35℃; Product distribution / selectivity;91.4%
With water In dichloromethane at 25 - 35℃; for 1.5h; Product distribution / selectivity;
pantoprazole sodium
138786-67-1

pantoprazole sodium

clcium {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

clcium {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

Conditions
ConditionsYield
Stage #1: pantoprazole sodium With sodium hydroxide In water at 25℃; for 1h;
Stage #2: With calcium chloride In water at 25℃; for 20h;
91.8%
pantoprazole sodium
138786-67-1

pantoprazole sodium

calcium bis{[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)-methylsulphinyl]-1H-benzimidazolide}

calcium bis{[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)-methylsulphinyl]-1H-benzimidazolide}

Conditions
ConditionsYield
With calcium chloride In water at 20℃; for 1.91667h;73%
pantoprazole sodium
138786-67-1

pantoprazole sodium

magnesium {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

magnesium {[5-(difluoromethoxy)]-2-[(3,4-dimethoxy-2-pyridinyl)methylsulphinyl]-1H-benzimidazolide} hydroxy

Conditions
ConditionsYield
Stage #1: pantoprazole sodium With sodium hydroxide In water at 25℃; for 0.25h;
Stage #2: With magnesium chloride In water at 25℃; for 2.5h;
52.7%
pantoprazole sodium
138786-67-1

pantoprazole sodium

magnesium bis[5-[difluoromethoxy]-2-[[3,4-dimethoxy-2-pyridinyl]-methylsulfinyl]-1H-benzimidazolide]

magnesium bis[5-[difluoromethoxy]-2-[[3,4-dimethoxy-2-pyridinyl]-methylsulfinyl]-1H-benzimidazolide]

Conditions
ConditionsYield
With magnesium chloride In water at 20 - 30℃; for 21 - 22h;
pantoprazole sodium
138786-67-1

pantoprazole sodium

pantoprazole sodium

pantoprazole sodium

Conditions
ConditionsYield
With sodium hydroxide In ethanol for 24h; Heating / reflux;
In tert-butyl methyl ether; acetonitrile at 20℃; for 48h;
at 100℃;
3-chlorosulfonylbenzoic acid 2-(toluene-4-sulfonyl)ethyl ester
651728-72-2

3-chlorosulfonylbenzoic acid 2-(toluene-4-sulfonyl)ethyl ester

pantoprazole sodium
138786-67-1

pantoprazole sodium

A

3-[5-difluoromethoxy-2-{(3,4-dimethoxy-pyridin-2-yl)-methanesulfinyl}-benzimidazole-1-sulfonyl]benzoic acid 2-(toluene-4-sulfonyl)ethyl ester

3-[5-difluoromethoxy-2-{(3,4-dimethoxy-pyridin-2-yl)-methanesulfinyl}-benzimidazole-1-sulfonyl]benzoic acid 2-(toluene-4-sulfonyl)ethyl ester

B

3-[6-difluoromethoxy-2-{(3,4-dimethoxy-pyridin-2-yl)-methanesulfinyl}-benzimidazole-1-sulfonyl]benzoic acid 2-(toluene-4-sulfonyl)ethyl ester
651728-78-8

3-[6-difluoromethoxy-2-{(3,4-dimethoxy-pyridin-2-yl)-methanesulfinyl}-benzimidazole-1-sulfonyl]benzoic acid 2-(toluene-4-sulfonyl)ethyl ester

Conditions
ConditionsYield
With sodium hydrogencarbonate; triethylamine In dichloromethane at 20℃; for 1.5h;
(4-chlorosulfonylphenoxy)acetic acid 2-(toluene-4-sulfonyl)ethyl ester
651728-13-1

(4-chlorosulfonylphenoxy)acetic acid 2-(toluene-4-sulfonyl)ethyl ester

pantoprazole sodium
138786-67-1

pantoprazole sodium

A

4-[5-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid 2-(toluene-4-sulfonyl)ethyl ester

4-[5-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid 2-(toluene-4-sulfonyl)ethyl ester

B

4-[6-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid 2-(toluene-4-sulfonyl)ethyl ester
651728-69-7

4-[6-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid 2-(toluene-4-sulfonyl)ethyl ester

Conditions
ConditionsYield
With sodium hydrogencarbonate; triethylamine In dichloromethane
With sodium hydrogencarbonate; triethylamine In dichloromethane Inert atmosphere;
pantoprazole sodium
138786-67-1

pantoprazole sodium

A

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H-benzimidazole
812664-93-0

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H-benzimidazole

B

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)chlorohydroxymethyl]sulfinyl]-1H-benzimidazole
812664-94-1

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)chlorohydroxymethyl]sulfinyl]-1H-benzimidazole

Conditions
ConditionsYield
With sodium hydroxide; sodium hypochlorite In water; acetonitrile at 20℃; for 12h;
pantoprazole sodium
138786-67-1

pantoprazole sodium

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole
102625-70-7

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole

Conditions
ConditionsYield
Stage #1: pantoprazole sodium With ethanol
Stage #2: With water
pantoprazole sodium
138786-67-1

pantoprazole sodium

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium salt monohydrate
797789-88-9

5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium salt monohydrate

Conditions
ConditionsYield
In acetone Purification / work up; Heating / reflux;
With water In ethyl acetate; acetone at 0 - 55℃; for 2.25h; Product distribution / selectivity;
With water In ethyl acetate at 0 - 5℃; for 2h; Product distribution / selectivity;
pantoprazole sodium
138786-67-1

pantoprazole sodium

pantoprazole sodium sesquihydrate

pantoprazole sodium sesquihydrate

Conditions
ConditionsYield
With water In ethyl acetate; acetone at 0 - 55℃; for 2.25h; Product distribution / selectivity;
With water In ethyl acetate at 0 - 5℃; for 2h; Product distribution / selectivity;
(4-chlorosulfonylphenoxy)acetic acid 2-(toluene-4-sulfonyl)ethyl ester
651728-13-1

(4-chlorosulfonylphenoxy)acetic acid 2-(toluene-4-sulfonyl)ethyl ester

pantoprazole sodium
138786-67-1

pantoprazole sodium

A

4-[6-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid sodium salt

4-[6-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid sodium salt

B

4-[5-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid sodium salt

4-[5-difluoromethoxy-2-{(3,4-dimethoxypyridin-2-yl)methanesulfinyl}benzimidazole-1-sulfonyl]phenoxyacetic acid sodium salt

Conditions
ConditionsYield
Stage #1: (4-chlorosulfonylphenoxy)acetic acid 2-(toluene-4-sulfonyl)ethyl ester; pantoprazole sodium With sodium hydrogencarbonate; triethylamine In dichloromethane Inert atmosphere;
Stage #2: With water; sodium hydrogencarbonate In acetonitrile at 65℃; for 5h; Inert atmosphere;
pantoprazole sodium
138786-67-1

pantoprazole sodium

β‐cyclodextrin
7585-39-9

β‐cyclodextrin

C16H14F2N3O4S(1-)*C42H70O35*Na(1+)

C16H14F2N3O4S(1-)*C42H70O35*Na(1+)

Conditions
ConditionsYield
In water

138786-67-1Relevant articles and documents

Synthetic method and application of pantoprazole sodium

-

Paragraph 0027-0028; 0031-0034; 0037-0040; 0043-0046; ..., (2021/07/28)

The invention belongs to the field of medicine synthesis, and discloses a synthesis method and application of pantoprazole sodium. The pantoprazole sodium is synthesized by the following steps: firstly carrying out sulfinylation on 5-difluoromethoxy-2-sulfenyl-1H-benzimidazole, and then carrying out Suzuki reaction on the 5-difluoromethoxy-2-sulfenyl-1H-benzimidazole and ((3, 4-dimethoxypyridine-2-yl) methyl) boric acid. According to the invention, the synthesis method of pantoprazole sodium provided by the invention can effectively improve the utilization rate of raw materials, improve the yield of intermediates and further reduce the production cost; the purification process of the synthesized intermediate and the final product in the synthesis method is simple, and the technological process is further shortened; and the synthesis method provided by the invention is suitable for synthesizing pantoprazole sodium, and the synthesized pantoprazole sodium is used for preparing a pantoprazole sodium injection.

Preparation of Pantoprazole sodium method and Pantoprazole sodium (by machine translation)

-

, (2019/02/27)

The invention relates to the preparation of Pantoprazole sodium method and pantoprazole sodium. In particular, the invention relates to a method of preparing pantoprazole sodium, comprising the following steps: 1) to 2 - hydroxymethyl - 3, 4 - dimethoxy pyridine (II) as the starting material, in under the action of chloride, the compound of formula III; 2) will be of the formula III compound in the presence of an inorganic base with 5 - difluoro - 2 - mercapto - 1 H - benzimidazole condensation, the compound of formula IV; 3) will be of the formula IV compound is oxidized by an oxidant generating 5 - difluoro - 2 - [(3, 4 - dimethoxy - 2 - pyridyl) methyl] sulfinyl - 1 H - benzimidazole is pantoprazole; 4) the obtained 5 - difluoro - 2 - [(3, 4 - dimethoxy - 2 - pyridyl) methyl] sulfinyl - 1 H - benzimidazole with sodium hydroxide reaction to produce salt that pantoprazole sodium (I); and optionally a 5) the resulting pantoprazole sodium is refined. The method of the invention said product has high purity, and the related impurities such as oxidation impurity, reducing the impurity, decomposition low impurity content. (by machine translation)

Method for refining pantoprazole sodium

-

Paragraph 0033; 0036; 0037; 0038; 0041; 0042; 0043; 0046, (2018/09/28)

The invention discloses a method for refining pantoprazole sodium. The method comprises the following steps: suspending a crude product of pantoprazole sodium in an ethanol-water mixed solution, adjusting the pH value to be 7.0-8.0 by using 1mol/L of hydrochloric acid, washing, and drying so as to obtain pantoprazole; dissolving pantoprazole into a mixed liquid of methanol and dichloromethane, dropping a sodium hydroxide-water solution, filtering a crystal, washing, and drying in vacuum, so as to obtain medicinal-grade pantoprazole sodium. The method is simple and convenient to operate, low inrefining cost and applicable to industrial amplification operation, and the prepared pantoprazole sodium is high in yield, high in purity, low in solvent residue, good in color and good in stability.

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