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1. (WO1991005564) SYNTHESIS AND USE OF AMINO ACID FLUORIDES AS PEPTIDE COUPLING REAGENTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/005564 International Application No.: PCT/US1990/006061
Publication Date: 02.05.1991 International Filing Date: 22.10.1990
Chapter 2 Demand Filed: 25.04.1991
IPC:
C07C 271/10 (2006.01) ,C07C 271/34 (2006.01) ,C07C 275/40 (2006.01) ,C07C 275/70 (2006.01) ,C07C 317/04 (2006.01) ,C07C 317/10 (2006.01) ,C07C 317/14 (2006.01) ,C07C 317/18 (2006.01) ,C07C 321/14 (2006.01) ,C07C 321/20 (2006.01) ,C07C 323/14 (2006.01) ,C07D 207/16 (2006.01) ,C07D 209/20 (2006.01) ,C07D 233/68 (2006.01) ,C07D 295/215 (2006.01) ,C07K 1/08 (2006.01) ,C07K 1/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
271
Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06
Esters of carbamic acids
08
having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10
with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
271
Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06
Esters of carbamic acids
32
having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
34
with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
40
being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
70
Compounds containing any of the groups e.g. isoureas
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
317
Sulfones; Sulfoxides
02
having sulfone or sulfoxide groups bound to acyclic carbon atoms
04
of an acyclic saturated carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
317
Sulfones; Sulfoxides
02
having sulfone or sulfoxide groups bound to acyclic carbon atoms
10
of an unsaturated carbon skeleton containing rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
317
Sulfones; Sulfoxides
14
having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
317
Sulfones; Sulfoxides
16
having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
18
with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
321
Thiols, sulfides, hydropolysulfides or polysulfides
12
Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms
14
of an acyclic saturated carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
321
Thiols, sulfides, hydropolysulfides or polysulfides
12
Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms
20
of an unsaturated carbon skeleton containing rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
10
containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
11
having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
14
the carbon skeleton being acyclic and unsaturated
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no 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
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
20
substituted additionally by nitrogen atoms, e.g. tryptophane
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
66
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
68
Halogen atoms
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
20
by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
215
Radicals derived from nitrogen analogues of carbonic acid
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
06
using protecting groups or activating agents
08
using activating agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
10
using coupling agents
Applicants:
RESEARCH CORPORATION TECHNOLOGIES, INC. [US/US]; 6840 East Broadway Boulevard Tucson, AZ 85710, US
Inventors:
CARPINO, Louis, A.; US
SADAT-AALAEE, Dean; US
Agent:
SCOTT, Anthony, C.; Scully, Scott, Murphy & Presser 400 Garden City Plaza Garden City, NY 11530, US
Priority Data:
426,12123.10.1989US
Title (EN) SYNTHESIS AND USE OF AMINO ACID FLUORIDES AS PEPTIDE COUPLING REAGENTS
(FR) SYNTHESE ET UTILISATION DE FLUORURES D'AMINOACIDES COMME REACTIFS ACCOUPLEURS DE PEPTIDES
Abstract:
(EN) A compound of formula (I) or the acid fluoride salts thereof, wherein BLK is an N-amino protecting group or hydrogen; AA is an amino acid residue and X is H or a protecting group, is useful as a coupling agent in peptide synthesis.
(FR) Un composé de la formule (I), ou ses sels de fluorure d'acide, où BLK est un groupe protecteur de N-amino ou hydrogène, AA est un résidu d'aminoacide, et X est H ou un groupe protecteur, est utile comme agent accoupleur lors de la synthèse des peptides.
Designated States: AU, CA, JP
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0496836US5750767CA2070419AU1991075885