# US 5,708,173 A · Heterocyclic compounds

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- Number: US 5,708,173 A
- Document ID: US5708173A
- Status: Granted
- Kind: A
- Application number: 08/660,393
- Filed: 1996-06-07
- Granted: 1998-01-13
- Earliest claimed: 1993-04-28
- Assignees: Fujisawa Pharmaceutical Co., Ltd.
- Inventors: Teruo Oku; Hiroshi Kayakiri; Shigeki Satoh; Yoshito Abe; Yuki Sawada; Takayuki Inoue; Hirokazu Tanaka
- Web page: https://patentgrep.com/patent/US5708173A

## CPC

- C07D 401/12: linked by a chain containing hetero atoms as chain links
- A61P 35/00: Antineoplastic agents
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 215/26: Alcohols; Ethers thereof
- C07D 237/28: Cinnolines
- C07D 239/74: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
- C07D 241/42: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D 401/14: containing three or more hetero rings
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07F 7/1804: {Compounds having Si-O-C linkages (Si-O-acyl linkages C07F7/1896)}
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

A compound of the formula: ##STR1## or its salt is prepared by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## Wherein the variables are all defined in claim 1.

## Claims

### Claim 1

A process for preparing a compound of the formula: ##STR9## where X.sup.1 is C--R.sup.6,
X.sup.2 is C--R.sup.7,
X.sup.3 is C--R.sup.8,
R.sup.1 is hydrogen or halogen.
R.sup.2 is halogen,
R.sup.3 is nitro, amino optionally having suitable substituent(s) or a heterocyclic group optionally having suitable substituent(s),
R.sup.4 and R.sup.5 are each hydrogen or halogen,
R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,
R.sup.7 is hydrogen or lower alkyl,
A is lower alkylene, and
Q is O or N--R.sup.9, in which R.sup.9 is hydrogen or acyl,
of its salt, which comprises:
a) reacting a compound of the formula: ##STR10## wherein R.sup.4, R.sup.5, X.sup.1, X.sup.2, X.sup.3 and Q are each as defined above, or its salt with a compound of the formula: ##STR11## wherein X is a leaving group, and
R.sup.1, R.sup.2, R.sup.3 and A are each as defined above or its salt.

### Claim 2

A process for preparing a compound of the formula: ##STR12## wherein X.sup.1 is C--R.sup.6,
X.sup.2 is C--R.sup.7,
X.sup.3 is C--R.sup.8,
R.sup.1 is hydrogen or halogen,
R.sup.2 is halogen,
R.sup.3 is nitro, amino optionally having suitable substituent(s) or a heterocyclic group optionally having suitable substituent(s),
R.sup.4 and R.sup.5 are each or halogen,
R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,
R.sup.7 is hydrogen or lower alkyl,
A is lower alkylene, and
Q is O or N--R.sup.9, in which R.sup.9 is hydrogen or acyl,
or its salt, which comprises;
a) reacting a compound of the formula: ##STR13## wherein R.sup.4, R.sup.5, X.sup.1, X.sup.2, X.sup.3 and Q are each as defined above,
or its salt with a compound of the formula: ##STR14## wherein X is a leaving group, and
R.sup.1, R.sup.2, R.sup.3 and A are each as defined above,
or its salt to give a compound of the formula: ##STR15## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X.sup.1, X.sup.2, X.sup.3, Q and A are each as defined above,
or its salt, or
b) acylating a compound of the formula: ##STR16## wherein R.sup.10 is hydrogen or lower alkyl, and
R.sup.1, R.sup.2, R.sup.4, R.sup.5, X.sup.1, X.sup.2, X.sup.3, Q and A are each as defined above,
or its salt to give a compound of the formula: ##STR17## wherein R.sup.11 is acyl, and
R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.10, X.sup.1, X.sup.2, X.sup.3, Q and A are each as defined above,
or its salt, or
c) acylating a compound of the formula: ##STR18## wherein R.sup.11 is acyl having amino, and
R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.10, X.sup.1, X.sup.2, X.sup.3, Q and A are each as defined above,
or its salt to give a compound of the formula: ##STR19## wherein R.sub.b.sup.11 is acyl having acylamino, and
R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.10, X.sup.1, X.sup.2, X.sup.3, Q and A are each as defined above,
or its salt, or
d) reacting a compound of the formula: ##STR20## wherein (AA) is amino acid residue,
Y is NH or lower alkenylene,
Z is CH or N, and
R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.10, X.sup.1, X.sup.2, X.sup.3, Q and A are each as defined above,
or its reactive derivative at the carboxy group
or a salt thereof with a compound of the formula: ##STR21## wherein R.sup.12 is hydrogen, lower alkyl, lower alkoxy(lower)alkyl, lower alkylamino(lower)alkyl, heterocyclic(lower)alkyl, a heterocyclic group, lower alkenyl, lower alkynyl, lower alkylcarbamoyloxy(lower)alkyl, lower alkoxycarbonyl(lower)alkyl, carboxy(lower)alkyl, lower alkylcarbamoyl(lower)alkyl, lower alkoxycarbonyl-ar(lower)alkyl, carboxy-ar(lower)alkyl, lower alkylcarbamoyl-ar(lower)alkyl, protected or unprotected hydroxy(lower)alkyl or aryl optionally substituted with lower alkylamino, and
R.sup.13 is hydrogen, lower alkyl, lower alkoxy(lower)alkyl or protected or unprotected hydroxy(lower)alkyl, or
R.sup.12 and R.sup.13 are taken together with the attached nitrogen atom to form a heterocyclic group optionally having suitable substituent(s),
or its reactive derivative at the amino group
or a salt thereof to give a compound of the formula: ##STR22## wherein R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.10, R.sup.12, R.sup.13, X.sup.1, X.sup.2, X.sup.3, A, (AA), Q, Y and Z are each as defined above,
or its salt.