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1. (WO1991008190) AMINO ACID PROTECTING GROUPS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/008190 International Application No.: PCT/US1990/007083
Publication Date: 13.06.1991 International Filing Date: 04.12.1990
Chapter 2 Demand Filed: 02.07.1991
IPC:
C07C 43/168 (2006.01) ,C07C 61/29 (2006.01) ,C07D 311/82 (2006.01) ,C07D 405/12 (2006.01) ,C07F 7/08 (2006.01) ,C07K 1/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
43
Ethers; Compounds having groups, groups or groups
02
Ethers
03
having all ether-oxygen atoms bound to acyclic carbon atoms
14
Unsaturated ethers
164
containing six-membered aromatic rings
168
containing six-membered aromatic rings and other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
61
Compounds having carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings
16
Unsaturated compounds
28
polycyclic
29
having a carboxyl group bound to a condensed ring system
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
78
Ring systems having three or more relevant rings
80
Dibenzopyrans; Hydrogenated dibenzopyrans
82
Xanthenes
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7
Compounds containing elements of the 4th Group of the Periodic System
02
Silicon compounds
08
Compounds having one or more C-Si linkages
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
06
using protecting groups or activating agents
Applicants:
RESEARCH CORPORATION TECHNOLOGIES, INC. [US/US]; 6840 East Broadway Boulevard Tucson, AZ 85710, US
Inventors:
CARPINO, Louis, A.; US
WU, An-Chuu; US
Agent:
SCOTT, Anthony, C.; Scully, Scott, Murphy & Presser 400 Garden City Plaza Garden City, NY 11530, US
Priority Data:
446,02105.12.1989US
Title (EN) AMINO ACID PROTECTING GROUPS
(FR) GROUPES DE PROTECTION D'AMINOACIDES
Abstract:
(EN) This invention relates to compounds of formula (I), wherein X is O, CR7R8, S or NR9 wherein R7 and R8 are independently hydrogen, or lower alkyl and R9 is lower alkyl; n is O or 1; R1 and R2 are independently hydrogen, lower alkyl, monoorganosilyl, triorganosilyl, halogen, aryl, or nitro; R3 is hydrogen, lower alkyl, monoorganosilyl, diorganosilyl, diorganosilyl, triorganosilyl, halogen, 9-fluorenylalkyl, cycloalkyl, aryl or aralkyl; R4 and R5 are independently hydrogen, lower alkyl, or aryl or one of R4 and R5 is 9-fluorenyl; R6 is H or COZ wherein Z is an amido acid, a peptide residue or a leaving group; and with the provisos that when n is O and R3 is hydrogen, R1 and R2 are not hydrogen, halogen or nitro; that when n is O and R3 is lower alkyl, R1 and R2 are not hydrogen, and that when X is O or CR7R8 wherein R7 and R8 are H; that R1, R2, R3, R4, R5, and R6 are not all simultaneously H. The compounds of the present invention are useful in peptide synthesis as blocking or protecting groups for reactive groups. The present invention is also directed to a method of protecting a reactive group of an organic molecule during a reaction which modifies a portion of the molecule other then the protected group.
(FR) Cette invention se rapporte à des composés de formule (I), dans laquelle X est O, CR7R8, S ou NR9 dans laquelle R7 et R8 sont indépendamment de l'hydrogène, ou un alcoyle inférieur, et R9 est un alcoyle inférieur; n est O ou 1; R1 et R2 sont indépendamment de l'hydrogène, un alcoyle inférieur, du monoorganosilyle, du diorganosilyle, du triorganosilyle, un halogène, un aryle ou nitro; R3 est de l'hydrogène, un alcoyle inférieur, du monoorganosilyle, du diorganosilyle, du triorganosilyle, de l'halogène, un fluorénylalcoyle-9, un cycloalcoyle, un aryle ou un aralcoyle; R4 et R5 sont indépendamment de l'hydrogène, un alcoyle, ou un aryle ou l'un de R4 et R5 est du fluorényle-9; R6 est H ou COZ dans lequel Z est un acide aminé, un résidu peptidique ou un groupe partant; et à condition que, lorsque n est O et R3 est hydrogène, R1 et R2 ne soient ni hydrogène, ni halogène, ni nitro; que lorsque n est O et R3 est un alcoyle inférieur, R1 et R1 ne soient pas hydrogène; et que lorsque X est O ou CR7R8 où R7 et R8 sont H, R1, R2, R3, R4, R5 et R6 ne soient pas tous simultanément H. Les composés selon la présente invention sont utiles dans la synthèse de peptides comme groupes de bloquage ou de protection pour des groupes réactifs. La présente invention se rapporte également à une méthode permettant de protéger un groupe réactif d'une molécule organique lors d'une réaction qui modifie une partie de la molécule qui ne fait pas partie du groupe de protection.
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:
AU1991069633