Process for preparing 4-arylamino-benzopyran and related compounds
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-233/02
C07D-233/04
C07D-233/54
출원번호
US-0486111
(1995-06-07)
발명자
/ 주소
Kronenthal David R. (Yardley PA) Mueller Richard H. (Ringoes NJ) Godfrey
Jr. Jollie D. (Trenton NJ)
출원인 / 주소
Bristol-Myers Squibb Company (Princeton NJ 02)
인용정보
피인용 횟수 :
2인용 특허 :
53
초록▼
A method of preparing compounds of the formula [Figure] I and pharmaceutically acceptable salts thereof which comprises converting a compound of the formula [Figure] II where the R2 substituent contains a hydrogen atom which is more acidic than the starred (*) hydrogen atom in formula II, to the cor
A method of preparing compounds of the formula [Figure] I and pharmaceutically acceptable salts thereof which comprises converting a compound of the formula [Figure] II where the R2 substituent contains a hydrogen atom which is more acidic than the starred (*) hydrogen atom in formula II, to the corresponding dianion of formula [Figure] IIA where M is a counterion preferably lithium or magnesium, using two equivalents of a base in an inert solvent such as tetrahydrofuran; then reacting compounds of formula IIA with an epoxide of formula [Figure] III to produce the compounds of formula I.
대표청구항▼
A process for preparing compounds of formula [Figure] I or pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or -N(O)-and the others are carbon atoms; Y is a single bond, -CH2-, -C(O)-, -O-, -S-or -N(R8)-; R1 is aryl or heterocy
A process for preparing compounds of formula [Figure] I or pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or -N(O)-and the others are carbon atoms; Y is a single bond, -CH2-, -C(O)-, -O-, -S-or -N(R8)-; R1 is aryl or heterocyclo; R2 is -COOR8, -CO-amino, -CO-substituted amino, amino, substituted amino, -NR8CO-amino, -NR8CO-substituted amino, -NR8COR9, -NR8SO2R9, -NR8(C〓NCN)-amino, -NR8(C〓NCN)-substituted amino, [Figure] -SR8, -SOR8, -SO2R8, -OR8l , cyano, heterocyclo, pyridine-N-oxide, [Figure] [Figure] (where Z is O or H2) or [Figure] R2 is hydroxy; R4 and R5 are each independently hydrogen, alkyl or arylalkyl, or R4 and R5 taken together with the carbon atom to which they are attached form a 5- to 7-membered carbocyclic ring; R6 is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, arylalkyl, (cycloalkyl)alkyl, -CN, -NO2, -COR8, -COOR8, -CONHR8, -CONR8R9, -CF3, -S-alkyl, -SOalkyl, -SO2alkyl, [Figure] halogen, amino substituted amino, -O-alkyl, -OCF3, -OCH2CF3, -OCOalkyl, -OCONR8alkyl, -NR8COalkyl, -NR8COOalkyl or -NR8CONR9, tetrazolyl, imidazole, oxazole, triazole or -S(O)2NR10R11; R7 is hydrogen, alkyl, hydroxy, -O-alkyl, amino, substituted amino, -NHCOR8, -CN or -NO2; or when R6 is -S(O)2NR10R11, then R7 in addition to the above is halogen, heterocyclo, haloalkyl or aryl; R8 and R9 are independently hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl; R10 and R11 are independently hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, haloalkyl, hydroxyalkyl, hydroxyalkyl substituted with a carboxylic ester or carboxylic acid, alkoxyalkyl, thioalkyl (cycloalkyl)alkyl, morpholinylalkyl, heterocyclo or (heterocyclo)alkyl; or R10 and R11 taken together with the nitrogen atom to which they are attached form a 5- to 7-membered mono or bicyclic ring, or 1-pyrrolidinyl, 1-piperidinyl, 1-azepinyl, 4-morpholinyl, 4-thiamorpholinyl, 4-thiamorpholine dioxide, 1-piperazinyl, 4-alkyl-1-piperazinyl, 4-arylalkyl-1-piperazinyl, 4-diarylalkyl-1-piperazinyl; or 1-piperazinyl, 1-pyrrolidinyl, 1-piperidinyl or 1-azepinyl substituted with one or more alkyl, alkoxy, alkylthio, halo, trifluoromethyl, hydroxy, aryl, arylalkyl, -COOR8 or -CO-substituted amino; or R10 and R7 taken together with the atoms to which they are attached form an unsubstituted 5- to 7-membered ring or a 5- to 7-membered ring substituted with aryl; X is alkyl; or X-R2 together are hydrogen, aryl or heterocyclo when R1 is heterocyclo; and n is an integer of 1 to 3; which comprises the steps of treating a compound of the formula [Figure] II (where the R2 substituent contains a hydrogen atom which is more acidic than the starred (*) hydrogen atom in formula II); with two equivalents of a base in an inert solvent, to form the corresponding dianion of formula [Figure] IIA where M is a counterion, then reacting the compounds of formula IIA with an epoxide of formula [Figure] III to produce the compounds of formula I.
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