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US4235820A Expired / Lapsed US ⏱️ 0.0 years remaining

Process for dibenzocycloheptene compounds

Assignee: Merck and Co Inc
•
Filing: 1976-08-10
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Granted: 1980-11-25
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Expires: 1996-08-10
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Abstract

Abstract This invention relates to a process for the preparation of 5H-dibenzo[a,d]cycloheptene compounds and derivatives having aminoalkyl substituents at the 5-position by reducing the corresponding 5-aminoalkyl-5-hydroxy compounds with an alkali metal borohydride in trifluoroacetic acid.

Inventors

  • 👤 Ben E. Evans

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 06:44
CPC Classifications
C; C07; C07C; C07C209/00; C07C209/68

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 48 words
A process for the reductive dehydroxylation of 5-(aminoalkyl or alkoxyalkyl)-5-hydroxy-5H-dibenzo[a,d]cycloheptene compound having one or more substituents or centers of unsaturation susceptible to catalytic hydrogenation which comprises contacting said 5H-dibenzo[a,d]cycloheptene compound with an alkali metal or ammonium borohydride in trifluoroacetic acid to produce the corresponding 5-(aminoalkyl or alkoxyalkyl)-5H-dibenzo[a,d]cycloheptene compound.
Claim 2
Dependent Claim 48 words
A process for the reductive dehydroxylation of 5-(aminoalkyl or alkoxyalkyl)-5-hydroxy-5H-dibenzo[a,d]cycloheptene compound having one or more substituents or centers of unsaturation susceptible to catalytic hydrogenation which comprises contacting said 5H-dibenzo[a,d]cycloheptene compound with an alkali metal or ammonium borohydride in trifluoroacetic acid to produce the corresponding 5-(aminoalkyl or alkoxyalkyl)-5H-dibenzo[a,d]cycloheptene compound.
Claim 3
Dependent Claim 201 words
A process according to claim 1 wherein the 5H-dibenzo[a,d]cycloheptene starting material is a compound of the formula ##STR7## wherein the dotted line is an optional added bond; Y is a loweralkoxy substituent or an amino substituent which may be mono- or dialkylated, e.g., ##STR8## X and X 2 are similar or dissimilar and are selected from hydrogen, an alkyl group having up to 6 carbon atoms, an alkenyl group having up to 6 carbon atoms, a perfluoroalkyl group having up to 4 carbon atoms, a phenyl or a substituted phenyl radical, an amino, an alkylamino group having up to 4 carbon atoms, a dialkylamino group having up to 8 carbon atoms, an alkylsulfonylamino group having up to 4 carbon atoms, halogen (fluorine, chlorine, bromine, or iodine), hydroxyl, an alkoxyl group having up to 4 carbon atoms, a perfluoroalkoxyl group having up to 4 carbon atoms, an alkylmercapto group having up to 4 carbon atonms, a perfluoroalkylmercapto group having up to 4 carbon atoms, an alkylsulfonyl group having up to 4 carbon atoms, a perfluoroalkylsulfonyl group having up to 4 carbon atoms, sulfamoyl, an alkylsulfamoyl group having up to 4 carbon atoms, or a dialkylsulfamoyl group having up to 8 carbon atoms.
Claim 4
Dependent Claim 18 words
A process according to claim 2 wherein the 5H-dibenzo[a,d]cycloheptene starting material is a compound of the formula: ##STR9##
Claim 5
Dependent Claim 14 words
A process according to claim 3 wherein the borohydride compound used is sodium borohydride.
Claim 6
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3-amino-5-(3-ethoxypropyl)-7-iodo-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is 3-amino-5-(3-ethoxypropyl)-7-iodo-5H-dibenzo[a,d]cycloheptene.
Claim 7
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3-amino-5-(3-ethoxypropyl)-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is 3-amino-5-(3-ethoxypropyl)-5H-dibenzo[a,d]cycloheptene.
Claim 8
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3,7-diiodo-5-(3-N,N-dimethylaminopropyl)-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is N,N-dimethyl-3-(3,7-diiodo-5H-dibenzo[a,d]cyclohepten-5-yl)propylamine.
Claim 9
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3-iodo-5-(3-N,N-dimethylaminopropyl)-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is N,N-dimethyl-3-(3-iodo-5H-dibenzo[a,d]cyclohepten-5-yl)propylamine.
Claim 10
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 5-(3-ethoxypropyl)-3-iodo-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is 5-(3-ethoxypropyl)-3-iodo-5H-dibenzo[a,d]cycloheptene.
Claim 11
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 5-(3-N,N-dimethylaminopropyl)-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is N,N-dimethyl-3-(5H-dibenzo[a,d]cyclohepten-5-yl)propylamine.
Claim 12
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3-bromo-5-(3-N,N-dimethylaminopropyl)-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction is N,N-dimethylamino-3(3-bromo-5H-dibenzo[a,d]cyclohepten-5-yl)propylamine.
Claim 13
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3-amino-5-(3-N,N-dimethylaminopropyl)-5H-dibenzo[a,d]cycloheptene and the product of the reaction is N,N-dimethyl-3(3-amino-5H-dibenzo[a,d]cyclohepten-5-yl)propylamine.
Claim 14
Dependent Claim 21 words
A process according to claim 4 wherein the 5H-dibenzo[a,d]cycloheptene starting material is 3-bromo-5-(3-ethoxypropyl)-5H-dibenzo[a,d]cyclohepten-5-ol and the product of the reaction of 3-bromo-5-(3-ethoxypropyl)-5H-dibenzo[a,d]cycloheptene.

References Cited (Backward Citations)

US3546228A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-11-25 1984-05-26 1984-11-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-11-25 1988-05-26 1988-11-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-11-25 1992-05-26 1992-11-25 $7700.00 Window Closed / Lapsed

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