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52763-21-0

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52763-21-0 Usage

Chemical Properties

white to brown crystalline powder

Uses

Ethyl 1-benzyl-3-oxo-4-piperidinecarboxylate hydrochloride was used in the synthesis of chromeno[3,4-c]pyridin-5-ones. It was used as building block for the syntheses of receptor agonists and antagonists. It was used as starting reagent in the synthesis of 4-amino-5-chloro-2-methoxy-N-[1-[5-(1-methylindol-3-ylcarbonylamino)pentyl]piperidin-4-ylmethyl]benzamide derivative.

Check Digit Verification of cas no

The CAS Registry Mumber 52763-21-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,2,7,6 and 3 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 52763-21:
(7*5)+(6*2)+(5*7)+(4*6)+(3*3)+(2*2)+(1*1)=120
120 % 10 = 0
So 52763-21-0 is a valid CAS Registry Number.
InChI:InChI=1/C15H19NO3/c1-2-19-15(18)13-8-9-16(11-14(13)17)10-12-6-4-3-5-7-12/h3-7,13H,2,8-11H2,1H3/p+1/t13-/m1/s1

52763-21-0 Well-known Company Product Price

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  • (Code)Product description
  • CAS number
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  • Detail
  • TCI America

  • (E0855)  Ethyl 1-Benzyl-3-oxo-4-piperidinecarboxylate Hydrochloride  >98.0%(T)

  • 52763-21-0

  • 1g

  • 340.00CNY

  • Detail
  • TCI America

  • (E0855)  Ethyl 1-Benzyl-3-oxo-4-piperidinecarboxylate Hydrochloride  >98.0%(T)

  • 52763-21-0

  • 5g

  • 1,200.00CNY

  • Detail
  • Alfa Aesar

  • (L07472)  1-Benzyl-4-ethoxycarbonyl-3-piperidone hydrochloride, tech. 90%   

  • 52763-21-0

  • 1g

  • 191.0CNY

  • Detail
  • Alfa Aesar

  • (L07472)  1-Benzyl-4-ethoxycarbonyl-3-piperidone hydrochloride, tech. 90%   

  • 52763-21-0

  • 5g

  • 633.0CNY

  • Detail
  • Aldrich

  • (143200)  Ethyl1-benzyl-3-oxo-4-piperidinecarboxylatehydrochloride  technical grade

  • 52763-21-0

  • 143200-5G

  • 999.18CNY

  • Detail
  • Aldrich

  • (143200)  Ethyl1-benzyl-3-oxo-4-piperidinecarboxylatehydrochloride  technical grade

  • 52763-21-0

  • 143200-25G

  • 3,693.69CNY

  • Detail

52763-21-0SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name Ethyl N-benzyl-3-oxo-4-piperidinecarboxylate hydrochloride

1.2 Other means of identification

Product number -
Other names ethyl 1-benzyl-3-oxopiperidine-4-carboxylate,hydrochloride

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:52763-21-0 SDS

52763-21-0Synthetic route

4-[benzyl(ethoxycarbonylmethyl)amino]butyric acid ethyl ester
63876-32-4

4-[benzyl(ethoxycarbonylmethyl)amino]butyric acid ethyl ester

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

Conditions
ConditionsYield
Stage #1: 4-[benzyl(ethoxycarbonylmethyl)amino]butyric acid ethyl ester With sodium ethanolate In toluene at 20 - 85℃; for 3.5h; Large scale;
Stage #2: With hydrogenchloride In water; toluene Large scale;
94%
Stage #1: 4-[benzyl(ethoxycarbonylmethyl)amino]butyric acid ethyl ester With sodium methylate In ethyl acetate for 4h; Reflux; Large scale;
Stage #2: With water; sodium hydroxide pH=7 - 8; Large scale;
Stage #3: With hydrogenchloride pH=1 - 2; Reagent/catalyst; Solvent; Large scale;
8.6 kg
ethyl 1-benzyl-3-oxo-4-piperidinecarboxylate
39514-19-7

ethyl 1-benzyl-3-oxo-4-piperidinecarboxylate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In ethanol at 22℃; for 0.5h; Inert atmosphere; Large scale;76.8%
4-bromoethylbutanoate
2969-81-5

4-bromoethylbutanoate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: triethylamine / 1,4-dioxane / 22 h / Reflux; Large scale
2.1: sodium ethanolate / toluene / 3.5 h / 20 - 85 °C / Large scale
2.2: Large scale
View Scheme
ethyl 2-(benzylamino)acetate
6436-90-4

ethyl 2-(benzylamino)acetate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: triethylamine / 1,4-dioxane / 22 h / Reflux; Large scale
2.1: sodium ethanolate / toluene / 3.5 h / 20 - 85 °C / Large scale
2.2: Large scale
View Scheme
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl 3-oxopiperidine-4-carboxylate
70637-75-1

ethyl 3-oxopiperidine-4-carboxylate

Conditions
ConditionsYield
In methanol; palladium dihydroxide100%
With hydrogen; palladium dihydroxide In dichloromethane at 20℃; under 3750.3 Torr; for 24h;84%
debenzylation;
di-tert-butyl dicarbonate
24424-99-5

di-tert-butyl dicarbonate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl 1-tert-butoxycarbonyl-3-oxopiperidine-4-carboxylate
71233-25-5

ethyl 1-tert-butoxycarbonyl-3-oxopiperidine-4-carboxylate

Conditions
ConditionsYield
With palladium 10% on activated carbon; hydrogen; triethylamine In methanol for 4h; Autoclave;100%
With palladium 10% on activated carbon; hydrogen; sodium carbonate In ethanol at 50℃; under 28502.9 Torr; for 48h; Autoclave;100%
With triethylamine; palladium-carbon In diethyl ether; ethanol94%
di-tert-butyl dicarbonate
24424-99-5

di-tert-butyl dicarbonate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

1-tert-butyl 4-ethyl 3-oxopiperidine-1,4-dicarboxylate
206111-40-2

1-tert-butyl 4-ethyl 3-oxopiperidine-1,4-dicarboxylate

Conditions
ConditionsYield
With Pd(OH)2/C; hydrogen; triethylamine In ethanol for 20h;100%
formamidine acetic acid
3473-63-0

formamidine acetic acid

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

7-benzyl-5,6,7,8-tetrahydro-3H-pyrido[3,4-d]pyrimidin-4-one
69981-00-6

7-benzyl-5,6,7,8-tetrahydro-3H-pyrido[3,4-d]pyrimidin-4-one

Conditions
ConditionsYield
With sodium ethanolate In ethanol for 2.5h; Inert atmosphere; Reflux; Large scale;100%
guanidine hydrogen carbonate
124-46-9, 20734-13-8, 100224-74-6, 593-85-1

guanidine hydrogen carbonate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

2-amino-7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(4aH)-one
62458-92-8

2-amino-7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(4aH)-one

Conditions
ConditionsYield
With sodium ethanolate for 16h; Heating / reflux;99%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

benzyl bromide
100-39-0

benzyl bromide

(SR)-1,4-dibenzyl-3-oxo-piperidine-4-carboxylic acid ethyl ester
312625-46-0

(SR)-1,4-dibenzyl-3-oxo-piperidine-4-carboxylic acid ethyl ester

Conditions
ConditionsYield
Stage #1: ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride With potassium tert-butylate In tetrahydrofuran at 0 - 20℃; Large scale;
Stage #2: benzyl bromide In tetrahydrofuran at 0 - 20℃; Large scale;
99%
With NaH; sodium hydrogencarbonate In water; N,N-dimethyl-formamide
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl 3-hydroxypiperidine-4-carboxylate
941571-79-5

ethyl 3-hydroxypiperidine-4-carboxylate

Conditions
ConditionsYield
With palladium 10% on activated carbon; hydrogen; triethylamine In ethanol at 20℃; under 760.051 Torr; for 48h;99%
Multi-step reaction with 2 steps
1: sodium tetrahydroborate / methanol / 3.75 h / 0 - 20 °C
2: hydrogen; 10 wt% Pd(OH)2 on carbon / ethanol / 14 h / 20 °C
View Scheme
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

cyclopropylcarboxamidine hydrochloride
57297-29-7

cyclopropylcarboxamidine hydrochloride

7-benzyl-2-cyclopropyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one

7-benzyl-2-cyclopropyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one

Conditions
ConditionsYield
With sodium methylate In methanol at 25℃; for 20h; Inert atmosphere;99%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl 1-benzyl-3-oxo-4-piperidinecarboxylate
39514-19-7

ethyl 1-benzyl-3-oxo-4-piperidinecarboxylate

Conditions
ConditionsYield
With sodium hydrogencarbonate In diethyl ether; water for 1h;96%
With sodium ethanolate In ethanol
With sodium hydrogencarbonate In ethyl acetate for 2h;
With sodium hydrogencarbonate In water; ethyl acetate at 20℃; for 0.5h;0.87 g
guanidine hydrochloride
50-01-1

guanidine hydrochloride

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

2-amino-7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(4aH)-one
62458-92-8

2-amino-7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(4aH)-one

Conditions
ConditionsYield
With sodium methylate In methanol at 100℃;96%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl 3-oxopiperidine-4-carboxylate hydrochloride

ethyl 3-oxopiperidine-4-carboxylate hydrochloride

Conditions
ConditionsYield
With 5% Pd(II)/C(eggshell); hydrogen In ethanol at 20℃; under 3750.38 Torr; for 4h;95%
With hydrogenchloride; palladium 10% on activated carbon; hydrogen In ethanol at 40℃; for 8h;91.4%
With hydrogen; palladium 10% on activated carbon In ethanol at 50℃; for 4h;84%
acetamidine hydrochloride
124-42-5

acetamidine hydrochloride

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

7-benzyl-2-methyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one
62259-92-1

7-benzyl-2-methyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one

Conditions
ConditionsYield
With sodium methylate In methanol at 25℃; for 20h; Inert atmosphere;95%
With sodium ethanolate In ethanol for 16h; Product distribution / selectivity; Heating / reflux;77%
With sodium ethanolate In ethanol; water; acetic acid17.1 g (95%)
Stage #1: acetamidine hydrochloride; ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride With sodium ethanolate In ethanol at 100℃; for 15h;
Stage #2: With hydrogenchloride In water pH=11; Product distribution / selectivity;
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl bromoacetate
105-36-2

ethyl bromoacetate

ethyl 1-benzyl-4-(2-ethoxy-2-oxoethyl)-3-oxopiperidine-4-carboxylate

ethyl 1-benzyl-4-(2-ethoxy-2-oxoethyl)-3-oxopiperidine-4-carboxylate

Conditions
ConditionsYield
Stage #1: ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride With potassium tert-butylate In tetrahydrofuran at 6 - 29℃; for 4h; Large scale;
Stage #2: ethyl bromoacetate In tetrahydrofuran at 10 - 20℃; for 29h; Large scale;
94%
di-tert-butyl dicarbonate
24424-99-5

di-tert-butyl dicarbonate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

1-tert-butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate
98977-34-5

1-tert-butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate

Conditions
ConditionsYield
With hydrogen; triethylamine; palladium(II) hydroxide/carbon In ethanol under 3102.97 Torr; for 5h;93%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

5-amino-3-methylthio-1,2,4-triazole
45534-08-5

5-amino-3-methylthio-1,2,4-triazole

A

8-benzyl-2-methylthio-6,7,8,9-tetrahydropyrido<3,4-d>-1,2,4-triazolo<1,5-a>pyrimidin-5(10H)-one
115549-85-4

8-benzyl-2-methylthio-6,7,8,9-tetrahydropyrido<3,4-d>-1,2,4-triazolo<1,5-a>pyrimidin-5(10H)-one

B

6-benzyl-2-methylthio-5,6,7,8-tetrahydropyrido<4,3-e>-1,2,4-triazolo<1,5-a>pyrimidin-9(10H)-one

6-benzyl-2-methylthio-5,6,7,8-tetrahydropyrido<4,3-e>-1,2,4-triazolo<1,5-a>pyrimidin-9(10H)-one

Conditions
ConditionsYield
In acetic acid for 6.5h; Heating;A 91%
B 2%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

1,1-dimethylguanidine dihydrogensulfate
311-77-3

1,1-dimethylguanidine dihydrogensulfate

7-benzyl-2-(dimethylamino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one

7-benzyl-2-(dimethylamino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one

Conditions
ConditionsYield
With sodium methylate In methanol at 25℃; for 20h; Inert atmosphere;90%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

thiourea
17356-08-0

thiourea

methyl iodide
74-88-4

methyl iodide

7-benzyl-5,6,7,8-tetrahydro-2-(methylthio)pyrido[3,4-d]pyrimidin-4(4aH)-one
871107-81-2

7-benzyl-5,6,7,8-tetrahydro-2-(methylthio)pyrido[3,4-d]pyrimidin-4(4aH)-one

Conditions
ConditionsYield
Stage #1: ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride; thiourea With sodium methylate In methanol at 100℃;
Stage #2: methyl iodide In methanol at 20℃; for 1h;
88%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

allyl bromide
106-95-6

allyl bromide

ethyl 1-benzyl-3-oxo-4-(prop-2-en-1-yl)piperidine-4-carboxylate

ethyl 1-benzyl-3-oxo-4-(prop-2-en-1-yl)piperidine-4-carboxylate

Conditions
ConditionsYield
Stage #1: ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride With potassium tert-butylate In tetrahydrofuran at 0 - 20℃; for 1h; Inert atmosphere;
Stage #2: allyl bromide In tetrahydrofuran at 0 - 20℃; Inert atmosphere;
84%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

urea
57-13-6

urea

7-benzyl-5,6,7,8-tetrahydropyridine[3,4-d]pyrimidine-2,4-diol
62459-02-3

7-benzyl-5,6,7,8-tetrahydropyridine[3,4-d]pyrimidine-2,4-diol

Conditions
ConditionsYield
With sodium In ethanol at 75℃; for 36h;83.2%
With ethanol; sodium at 75℃; for 36h;83.2%
With ethanol; sodium at 90℃; for 12h;62%
With ethanol; sodium at 80℃; for 20h;62%
With sodium methylate In methanol; ethanol for 4h; Reflux;
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

6-benzyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-ol
909187-64-0

6-benzyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-ol

Conditions
ConditionsYield
With hydrazine hydrate; triethylamine In ethanol at 80℃; for 1.5h;83%
With hydrazine at 20℃; for 48h;
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

5-amino-3-methylthio-1,2,4-triazole
45534-08-5

5-amino-3-methylthio-1,2,4-triazole

8-benzyl-2-methylthio-6,7,8,9-tetrahydropyrido[3,4-d][1,2,4]triazolo[1,5-a]pyrimidin-5(10H)-one monohydrochloride

8-benzyl-2-methylthio-6,7,8,9-tetrahydropyrido[3,4-d][1,2,4]triazolo[1,5-a]pyrimidin-5(10H)-one monohydrochloride

Conditions
ConditionsYield
With acetic acid for 8h; Condensation; Heating;81%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

urea
57-13-6

urea

7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine-2,4(1H,3H)-dione
62459-02-3

7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine-2,4(1H,3H)-dione

Conditions
ConditionsYield
With sodium methylate In ethanol for 17h; Heating / reflux;80%
With sodium methylate In methanol for 18h; Reflux; Inert atmosphere;58.3%
With sodium methylate In methanol at 0℃; for 20h; Reflux; Inert atmosphere;
benzamidine monohydrochloride
1670-14-0

benzamidine monohydrochloride

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

C20H19N3O
62259-93-2

C20H19N3O

Conditions
ConditionsYield
With sodium methylate In methanol; ethanol at 0℃; Heating / reflux;80%
2-methylisothiourea sulphate
14527-26-5, 867-44-7

2-methylisothiourea sulphate

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

7-benzyl-2-(methylthio)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-ol

7-benzyl-2-(methylthio)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-ol

Conditions
ConditionsYield
With sodium methylate In methanol at 20℃; for 12h;80%
formamidine acetic acid
3473-63-0

formamidine acetic acid

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

7-benzyl-5,6,7,8-tetrahydro-3H-pyrido[3,4-d]pyrimidin-4-one
62458-96-2

7-benzyl-5,6,7,8-tetrahydro-3H-pyrido[3,4-d]pyrimidin-4-one

Conditions
ConditionsYield
With sodium methylate In methanol at 25℃; for 20h; Inert atmosphere;79%
Stage #1: formamidine acetic acid; ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride With sodium methylate In methanol at 25℃; for 20h;
Stage #2: With acetic acid In methanol; water at 0 - 25℃;
79%
With sodium methylate In methanol at 20℃; for 20h;70%
Stage #1: formamidine acetic acid; ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride With sodium methylate In methanol at 20℃; for 20h;
Stage #2: With acetic acid In methanol; water at 0 - 20℃; for 1h;
70%
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

7-benzyl-2-(trifluoromethyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-ol
647862-97-3

7-benzyl-2-(trifluoromethyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-ol

Conditions
ConditionsYield
With sodium ethanolate In ethanol at 20 - 80℃; for 17.25h;78%
With ethanol; sodium at 20 - 80℃; for 17h; Inert atmosphere;78%
With sodium ethanolate In ethanol at 20℃; for 31.25h;
Stage #1: ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride; trifluoroacetamidine With sodium ethanolate at 20℃; for 1.25h;
Stage #2: for 30h; Heating / reflux;
With sodium ethanolate In ethanol for 31.25h; Heating / reflux;
ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

ethyl 2-amino-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylate
911010-88-3

ethyl 2-amino-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylate

Conditions
ConditionsYield
With ammonium acetate In ethanol at 20℃; for 1h;75%
With ammonium acetate In ethanol at 20℃; for 1h;
With ammonium acetate In ethanol at 20℃; for 3h;29.2 g
With ammonium acetate In ethanol at 20℃; for 3h;29.2 g
5-amino-3-morpholino-1H-1,2,4-triazole
51420-46-3

5-amino-3-morpholino-1H-1,2,4-triazole

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride
52763-21-0

ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride

A

8-benzyl-2-morpholino-6,7,8,9-tetrahydropyrido<3,4-d>-1,2,4-triazolo<1,5-a>pyrimidin-5(10H)-one
115549-86-5

8-benzyl-2-morpholino-6,7,8,9-tetrahydropyrido<3,4-d>-1,2,4-triazolo<1,5-a>pyrimidin-5(10H)-one

B

6-benzyl-2-morpholino-5,6,7,8-tetrahydropyrido<4,3-e>-1,2,4-triazolo<1,5-a>pyrimidin-9(10H)-one

6-benzyl-2-morpholino-5,6,7,8-tetrahydropyrido<4,3-e>-1,2,4-triazolo<1,5-a>pyrimidin-9(10H)-one

Conditions
ConditionsYield
In acetic acid for 7h; Heating;A 72%
B 3%

52763-21-0Relevant articles and documents

Preparation method of N-benzyl-3-oxopiperidine-4-carboxylic acid ethyl ester hydrochloride

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Paragraph 0006; 0018; 0022-0026; 0030-0034; 0038-0041, (2020/02/10)

The invention provides a preparation method of N-benzyl-3-oxopiperidine-4-carboxylic acid ethyl ester hydrochloride, and the method comprises the following steps: (1) preparing an intermediate 2: dissolving N-benzyl glycine ethyl ester in an organic solvent, adding 4-halogenated ethyl butyrate and alkali, and reacting to obtain N-benzyl glycine ethyl ester; (2) dissolving the intermediate 2 in anorganic solvent, reacting with alkali, adjusting the pH value to 7-8 after the reaction is finished, adding water for washing, adjusting the pH value of an organic layer to 1-2, and separating out crystals to obtain a crude product; and (3) dissolving the crude product in water, adding alkali to adjust the pH value to 7-8, adding an organic solvent to extract, washing, adjusting the pH value of anorganic layer to 1-2, and crystallizing to obtain the product. The method is simple in process operation, high in product yield, high in purity and easy for industrial production.

Efficient enantioselective synthesis of the NMDA 2B receptor antagonist Ro 67-8867

Scalone, Michelangelo,Waldmeier, Pius

, p. 418 - 425 (2013/09/06)

An efficient, enantioselective, and scalable eight-step synthesis for the NMDA 2B receptor antagonist Ro 67-8867 (S,S)-1 selected for the treatment of acute ischemie stroke is described based on the coupling reaction of the amino alcohol (S,S)-6 with the sulfone building block 7. The synthesis of the amino alcohol (S,S)-6 was achieved by the highly selective asymmetric hydrogenation of the piperidinone 4*HCl proceeding with concomitant dynamic kinetic resolution to (S,S)-5. Subsequent debenzylation afforded the enantiomerically pure amino alcohol (S,S)-6 after ee-enhancement by simple crystallization in good yield. The hydrogenation substrate 4*HCl was prepared as a stable hydrochloride in two steps from ethyl N-benzyl-3-oxo-4-piperidinecarboxylate hydrochloride (2) for which a new, short, efficient, and cheap synthesis was developed. To bypass a mutagenic intermediate, a revised safe protocol for the sulfone building block 7 was established. The new synthesis allows the access to Ro 67-8867 (S,S)-1 in an overall yield of 53% compared to 3.5% of the Discovery Chemistry approach.

Ethanesulfonyl-piperidine derivatives

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, (2008/06/13)

The invention relates to compounds of the general formula STR1whereinR 1 signifies hydrogen or hydroxy; R 2 signifies hydrogen or methyl; and X signifies --O-- or --CH 2 -- and their pharmaceutically acceptable acid addition salts.It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer''s disease, Parkinson''s disease, Huntington''s disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

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