The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I)
wherein R
1
is a hydrogen atom and the like; R
2
is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R
3
is unsubstituted (i.e., absence), a hydrogen atom and the like; R
4
and R
5
are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R
6
is (cyclic group optionally having substituent(s))-carbonyl, and the like; R
7
, R
8
, R
9
and R
10
are the same or different and each is a hydrogen atom, halogen and the like; or R
7
and R
8
, R
8
and R
9
, and R
9
and R
10
may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;
--- represents unsubstituted (i.e., absence) or a single bond; and
represents a single bond or a double bond, or a salt thereof, and the like.
Process for the preparation of aryl ketones generating reduced amounts of toxic byproducts
申请人:College of the Holy Cross
公开号:US06362375B1
公开(公告)日:2002-03-26
An efficient, cost-effective method useful for the production of aryl ketones that minimizes the generation of toxic byproducts is disclosed. The method utilizes a metal triflate salt to catalyze the reaction between the carboxylic acid substrate and the aromatic substrate. The water generated by the reaction is collected and removed during the process.
A compound represented by the formula (I)
wherein A is a benzene ring optionally having substituent(s), R is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group optionally having substituent(s), X1 and X2 are each a bond or a divalent C
1-5
chain hydrocarbon group optionally having substituent(s), X3 is a methylene group having substituent(s), Y is a bond or the like, and Z is a hydrocarbon group optionally having substituent(s) or the like, or a salt thereof. The compound of the present invention or a salt thereof is useful as an NK receptor antagonist.
The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I)
wherein R
1
is a hydrogen atom and the like; R
2
is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R
3
is unsubstituted (i.e., absence), a hydrogen atom and the like; R
4
and R
5
are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R
6
is (cyclic group optionally having substituent(s))-carbonyl, and the like; R
7
, R
8
, R
9
and R
10
are the same or different and each is a hydrogen atom, halogen and the like; or R
7
and R
8
, R
8
and R
9
, and R
9
and R
10
may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; —
--- represents unsubstituted (i.e., absence) or a single bond; and
represents a single bond or a double bond, or a salt thereof, and the like.
The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I)
wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;
--- represents unsubstituted (i.e., absence) or a single bond; and
represents a single bond or a double bond, or a salt thereof, and the like.