Journal of Chemical Research

An improved synthesis of a β-blocker celiprolol hydrochloride

L Ji, XY Mao, C Qian, XZ Chen

Index: Ji, Li; Qian, Chao; Chen, Xin-Zhi; Mao, Xiao-Yuan 2011 , vol. 35, # 11 p. 640 - 643,4

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Citation Number: 0

Abstract

Celiprolol hydrochloride, a β-blocker drug, has been synthesised from 4- chloronitrobenzene. The route involved hydrolysis of the chloride and acetylation of the phenol, reduction of the nitro group, and acylation of theamine. This was followed by Fries rearrangement of the acetyl group, Williamson etherification with epichlorohydrin, followed by opening of the epoxide ring and salt formation. The overall yield of celipropol was 39.1 ...

 Related Synthetic Route
4-Chloronitrobenzene Structure

100-00-5

4-Chloronitrobenzene

~%

(4-Aminophenyl)acetic acid Structure

13871-68-6

(4-Aminophenyl)...

Ethanoic anhydride Structure

108-24-7

Ethanoic anhydride

4-Chloronitrobenzene Structure

100-00-5

4-Chloronitrobenzene

~90%

P-NITROPHENYLACETATE Structure

830-03-5

P-NITROPHENYLACETATE

4-(3,3-diethylureido)phenyl acetate Structure

1357457-94-3

4-(3,3-diethylu...

~%

3-(3-acetyl-4-(oxiran-2-ylmethoxy)phenyl)-1,1-diethylurea Structure

56980-98-4

3-(3-acetyl-4-(...

4-Chloronitrobenzene Structure

100-00-5

4-Chloronitrobenzene

~%

3-(3-acetyl-4-(oxiran-2-ylmethoxy)phenyl)-1,1-diethylurea Structure

56980-98-4

3-(3-acetyl-4-(...

P-NITROPHENYLACETATE Structure

830-03-5

P-NITROPHENYLACETATE

~%

3-(3-acetyl-4-(oxiran-2-ylmethoxy)phenyl)-1,1-diethylurea Structure

56980-98-4

3-(3-acetyl-4-(...

(4-Aminophenyl)acetic acid Structure

13871-68-6

(4-Aminophenyl)...

~%

3-(3-acetyl-4-(oxiran-2-ylmethoxy)phenyl)-1,1-diethylurea Structure

56980-98-4

3-(3-acetyl-4-(...

celiprolol Structure

56980-93-9

celiprolol

~80%

Celiprolol HCl Structure

57470-78-7

Celiprolol HCl

4-(3,3-diethylureido)phenyl acetate Structure

1357457-94-3

4-(3,3-diethylu...

~87%

N'-(3-acetyl-4-hydroxyphenyl)-N,N-diethyl urea Structure

79881-89-3

N'-(3-acetyl-4-...

4-Chloronitrobenzene Structure

100-00-5

4-Chloronitrobenzene

~%

N'-(3-acetyl-4-hydroxyphenyl)-N,N-diethyl urea Structure

79881-89-3

N'-(3-acetyl-4-...

P-NITROPHENYLACETATE Structure

830-03-5

P-NITROPHENYLACETATE

~%

N'-(3-acetyl-4-hydroxyphenyl)-N,N-diethyl urea Structure

79881-89-3

N'-(3-acetyl-4-...

(4-Aminophenyl)acetic acid Structure

13871-68-6

(4-Aminophenyl)...

~%

N'-(3-acetyl-4-hydroxyphenyl)-N,N-diethyl urea Structure

79881-89-3

N'-(3-acetyl-4-...

tert-Butylamine Structure

75-64-9

tert-Butylamine

3-(3-acetyl-4-(oxiran-2-ylmethoxy)phenyl)-1,1-diethylurea Structure

56980-98-4

3-(3-acetyl-4-(...

~%

celiprolol Structure

56980-93-9

celiprolol


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