US 2018/0008583 A1Published application

Method for manufacturing novel nitrogen-containing compound or salt thereof and manufacturing intermediate of novel nitrogen-containing compound or salt thereof

AssigneeFUJIFILM Corporation

InventorsHirofumi FUKUNAGA, Sachiko SHINJO, Daisuke NAKAGAWA, Shinichiro SEKINE, Takayuki YAMAKAWA

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Abstract

Provided are a method for efficiently manufacturing a nitrogen-containing compound, which is used for manufacturing a treatment agent for integrin-related diseases, or a salt thereof and a manufacturing intermediate of the compound or a salt thereof. A method for manufacturing a novel nitrogen-containing compound or a salt thereof includes (1) a step of obtaining a compound represented by Formula [10] or a salt thereof through an amidation reaction; and (2) a step of deprotecting the compound represented by Formula [10] or a salt thereof.

Claims18

Dependent claims

A method for manufacturing a compound represented by Formula [11] or a salt thereof, comprising:

(1) a step of reacting a compound represented by Formula [1] or a salt thereof
(in the formula, R1 represents a hydrogen atom or an amino-protecting group;
R2 represents a carboxyl-protecting group;
L1 represents a group represented by Formula [2a]
(in the formula, R3a, R4a, R5a, and R6a are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group;
p1 represents an integer of 1 to 3;
q1 represents an integer of 0 to 3;
and r1 represents an integer of 1 to 6);
L2 represents a group represented by Formula [2b]
(in the formula, R3b, R4b, R5b, and R6b are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group;
p2 represents an integer of 1 to 3;
q2 represents an integer of 0 to 3;
and r2 represents an integer of 1 to 6)) with a compound represented by Formula [3] or a salt thereof
(in the formula, L3 represents a group represented by Formula [2c]
(in the formula, R3c, R4c, R5c, and R6c are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group;
p3 represents an integer of 1 to 3;
q3 represents an integer of 0 to 3;
and r3 represents an integer of 1 to 6);
A1 represents any one of the groups represented by Formulae [4] to [9]
(in the formulae, * represents a binding position;
and R7's are the same as or different from each other and represent a carboxyl-protecting group);
and m represents an integer of 1 to 3)) so as to obtain a compound represented by Formula [10] or a salt thereof;
(in the formula, R1, R2, L1, L2, L3, A1, and m have the same definition as R1, R2, L1, L2, L3, A1, and m described above);
and
(2) a step of deprotecting the compound represented by Formula [10] or a salt thereof,
(in the formula, A2 represents any one of the groups represented by Formulae [12] to [17]
(in the formulae, * represents a binding position);
and L1, L2, L3, and m have the same definition as L1, L2, L3, and m described above).

25 more elements

A compound represented by Formula [19] or a salt thereof

(in the formula, R1 represents a hydrogen atom or an amino-protecting group;
R8 represents a C2-6 alkyl group which may be substituted or a benzyl group which may be substituted;
R9 represents a hydrogen atom, an amino-protecting group, or a group represented by Formula [20]
(in the formula, * represents a binding position;
R10 represents a hydroxyl group or a group represented by Formula [21]
(in the formula, * represents a binding position, L3 represents a group represented by Formula [2c]
(in the formula, R3c, R4c, R5c, and R6c are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group;
p3 represents an integer of 1 to 3;
q3 represents an integer of 0 to 3;
and r3 represents an integer of 1 to 6);
A1 represents any one of the groups represented by Formulae [4] to [9]
(in the formulae, * represents a binding position;
and R7 represents a carboxyl-protecting group);
and m represents an integer of 1 to 3);
L2 represents a group represented by Formula [2b]
(in the formula, R3b, R4b, R5b, and R6b are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group;
p2 represents an integer of 1 to 3;
q2 represents an integer of 0 to 3;
and r2 represents an integer of 1 to 6);
and L1 represents a group represented by Formula [2a]
(in the formula, R3a, R4a, R5a, and R6a are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group;
p1 represents an integer of 1 to 3;
q1 represents an integer of 0 to 3;
and r1 represents an integer of 1 to 6)).

21 more elements

Dependencies are inferred from the claim text.

Facts

Application: 15/712,815Filed 22 Sep 2017
Priority: JP 2015-06230625 Mar 2015
Published: 11 Jan 2018
Term ends: Not estimatedThe source records don’t support an estimate.

Classification27 codes

A61K 31/4375
Ortho- or peri-condensed with heterocyclic ring systems: the heterocyclic ring system containing a six-membered ring having nitrogen as a ring…
A61K 31/145
Amines: having sulfur, e.g. thiurams , Sulfinylamines , Sulfonylamines
A61K 31/223
Of acyclic acids, e.g. pravastatin: of alpha-aminoacids
A61K 31/27
Esters, e.g. nitroglycerine, selenocyanates: of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine