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1. (WO1987003584) SYNTHESIS OF OPTICALLY ACTIVE ARYLOXYPROPANOLAMINES AND ARYLETHANOLAMINES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1987/003584 International Application No.: PCT/US1986/002407
Publication Date: 18.06.1987 International Filing Date: 14.11.1986
IPC:
C07D 209/08 (2006.01) ,C07D 209/30 (2006.01) ,C07D 209/52 (2006.01) ,C07D 209/88 (2006.01) ,C07D 215/227 (2006.01) ,C07D 235/26 (2006.01) ,C07D 237/20 (2006.01) ,C07D 239/545 (2006.01) ,C07D 261/08 (2006.01) ,C07D 285/10 (2006.01) ,C07D 295/195 (2006.01) ,C07D 307/12 (2006.01) ,C07D 307/46 (2006.01) ,C07D 307/80 (2006.01) ,C07D 307/88 (2006.01) ,C07D 311/20 (2006.01) ,C07D 335/06 (2006.01) ,C07D 473/08 (2006.01) ,C07D 493/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
08
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
30
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
52
condensed with a ring other than six-membered
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56
Ring systems containing three or more rings
80
[b, c]- or [b, d]-condensed
82
Carbazoles; Hydrogenated carbazoles
88
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20
Oxygen atoms
22
attached in position 2 or 4
227
only one oxygen atom which is attached in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
24
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
26
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
237
Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
02
not condensed with other rings
06
having three double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20
Nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
52
Two oxygen atoms
54
as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
545
with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
261
Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02
not condensed with other rings
06
having two or more double bonds between ring members or between ring members and non-ring members
08
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
10
1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16
acylated on ring nitrogen atoms
18
by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
195
Radicals derived from nitrogen analogues of carboxylic acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
10
with substituted hydrocarbon radicals attached to ring carbon atoms
12
Radicals substituted by oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
38
with substituted hydrocarbon radicals attached to ring carbon atoms
40
Radicals substituted by oxygen atoms
46
Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77
ortho- or peri-condensed with carbocyclic rings or ring systems
78
Benzo [b] furans; Hydrogenated benzo [b] furans
79
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
80
Radicals substituted by oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77
ortho- or peri-condensed with carbocyclic rings or ring systems
87
Benzo [c] furans; Hydrogenated benzo [c] furans
88
with one oxygen atom directly attached in position 1 or 3
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
311
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02
ortho- or peri-condensed with carbocyclic rings or ring systems
04
Benzo [b] pyrans, not hydrogenated in the carbocyclic ring
06
with oxygen or sulfur atoms directly attached in position 2
20
hydrogenated in the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
335
Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
04
condensed with carbocyclic rings or ring systems
06
Benzothiopyrans; Hydrogenated benzothiopyrans
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
04
two oxygen atoms
06
with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
08
with methyl radicals in positions 1 and 3, e.g. theophylline
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
493
Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants:
E.I. DU PONT DE NEMOURS AND COMPANY [US/US]; 1007 Market Street Wilmington, DE 19898, US
Inventors:
MAI, Khuong, H., X.; US
PATIL, Ghanshyam; US
MATIER, William, L.; US
Agent:
FATO, Gildo, E.;; Du Pont Critical Care, Subsidiary of E.I. Du Pont de Nemours & Co., (INC.); 1600 Waukegan Road; Waukegan, IL 60085, US
Priority Data:
804,40704.12.1985US
Title (EN) SYNTHESIS OF OPTICALLY ACTIVE ARYLOXYPROPANOLAMINES AND ARYLETHANOLAMINES
(FR) SYNTHESE D'ARYLOXYPROPANOLAMINES ET ARYLETHANOLAMINES OTPIQUEMENT ACTIVES
Abstract:
(EN) A process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of formula (1) or (2), wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is -NR2COR3, -NR2CONR3R4, -NR2SO2R3, -NR2SO2NR3R4, or -NR2COOR5, where R2, R3, R4, and R5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R3 and R5 are not hydrogen when B is -NR2SO2R3 or -NR2COOR5, or R3 and R4 may together with N form a 5- to 7-membered heterocyclic group. The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.
(FR) Procédé de préparation d'une aryloxypropanolamine (1) ou d'une aryléthanolamine (2) racémique ou chirale de formule (1) ou (2) dans lesquelles Ar représentent un aryle, un aryle substitué, un hétéroaryle ou un aralkyle et R représente un alkyle, un alkyle substitué, un aralkyle, ou WB, W représentant un alkylène à chaîne droite ou ramifiée et ayant entre 1 et environ 6 atomes de carbone et B représentant -NR2COR3, -NR2CONR3R4 -NR2SO2R3, -NR2SO2NR3R4, ou -NR2COOR5, où R2, R3, R4 et R5 peuvent être identiques ou différents et peuvent représenter un hydrogène, un alkyle, un alkoxyalkyle, un alkoxyaryle, un cycloalkyle, un alkynyle, un aryle, un hétéroaryle ou un aralkyle, à l'exception que R3 et R5 ne représentent pas l'hydrogène lorsque B représente -NR2SO2R3 ou -NR2COOR5, ou R3 et R4 peuvent former ensemble avec N un groupe hétérocyclique à 5 ou 7 membres. Le procédé peut être utilisé pour préparer des agents bêta-bloquants utiles dans le traitement d'états cardiaques.
Designated States: AU, JP
European Patent Office (CH, DE, FR, GB, IT, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0249610AU1986066287AU1989046863