Method of preparing derivatives of alkanolamine or their salts
专利摘要:
1436173 Mono ethers of dehydroxy amines HASSLE AB 4 July 1973 [6 July 1972] 31869/73 Heading C2C Novel compounds of Formula I wherein R<SP>1</SP> is a C 1 -C 4 alkyl or hydroxy-C 1 -C 4 alkyl group, R<SP>2</SP> is a carbamoylamino-C 1 -C 4 alkyl, mono- or di-C 1 -C 4 alkylcarbamoylamino-C 1 -C 4 alkyl, carbamoylamino-C 1 -C 4 alkoxy, mono- or di-C 1 -C 4 alkylcarbamoylamino - C 1 -C 4 alkoxy, carbamoyloxy - C 1 -C 4 alkyl, mono- or di-C 1 -C 4 alkylcarbamoyloxy- C 1 -C 4 alkyl, carbamoyloxy-C 1 -C 4 alkoxy or mono- or di-C 1 -C 4 alkylcarbamoyloxy-C 1 -C 4 alkoxy group and R<SP>3</SP> is a hydrogen or halogen atom or a C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, (C 1 -C 4 alkoxy)methyl, C 1 -C 4 alkoxy, C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, C 1 -C 4 alkylthio, C 2 -C 4 alkenylthio, C 2 -C 4 alkynlthio or C 1 -C 4 acyl groups are prepared by one of the following methods (a) and amine R<SP>1</SP>NH 2 is reacted with a compound of formula wherein X<SP>1</SP> is OH and Z is reactive esterified OH or X<SP>1</SP> and Z form an epoxy group; (b) a compound R<SP>1</SP>Z is reacted with an amine of formula (c) a compound of formula is reacted with a compound of formula (V) reduction of a compound selected from formulµ (d) by hydrolysis of a derivative which has an arylsulphonyl, benzoyl, cyano, silyl alkylidene benzylidene, phosphorylidene or substituted methylene substituent at the nitrogen atom of the amino group and/or at the hydroxy group, or reducing such a derivative having an arylsulphonyl substituent at the nitrogen atom or hydroxy group; (e) hydrogenation of a compound of formula or (f) by converting a group X<SP>2</SP> in a compound of Formula XI wherein X<SP>2</SP> is a hydroxyalkyl-, esterified hydroxyalkyl-, hydroxyalkoxy-, esterified hydroxyalkoxy-, hydroxy-, aminoalkyl-, aminoalkoxy-, alkanoylaminoalkyl-, alkanoylaminoalkoxy-, alkanoyloxyalkyl-, alkanoyloxyalkoxy-, aminothiocarbamylaminoalkyl-, aminothiocarbamylaminoalkoxy-, alkylaminothiocarbamylaminoalkyl-, alkylaminothiocarbamylaminoalkoxy-, imino(halo)carbaminoalkyl-, imino(halo)carbaminoalkoxy-, iminocarbiminoalkyl-, or iminocarbiminoalkoxygroup into a group as defined for R<SP>2</SP> in claim 1, using a method known per se for effecting such a conversion. Pharmaceutical compositions in conventional forms for oral, rectal or parenteral and having #-blocking activity comprise an above novel compound and a carrier or diluent. 公开号:SU841581A3 申请号:SU742029435 申请日:1974-06-03 公开日:1981-06-23 发明作者:Бернхард Бернтссон Педер;Элоф Брендстрем Арне;Ингемар Карлссон Энар;Эк Ларс;Роджер Самуэльссон Бенни;Эрик Сестранд Свен;Кристер Страндлунд Герт;Арне Хяльмар Аблад Бернт 申请人:Аб Хессле (Фирма); IPC主号:
专利说明:
one This invention relates to a process for the preparation of alkanolamine derivatives having formacological activity. Methods are known for the preparation of various alkanolamine derivatives, which as a rule are used in medicine, in particular, as fiadrenergic receptors. The known method l for the preparation of alkanolamines of the general formula in the hydroxy ester, R has the meaning given in formula (1). The purpose of the invention is to expand the range of products that affect living organisms. The goal is achieved by the method of obtaining alkanolamines of the general formula -OCH, CHOHCH-NH-Rf (I)
权利要求:
Claims (1) [1] Claim A method of producing alkanolamine derivatives of the general formula OCH 2 SNONCH g - NH - r 'where R 1 is isopropyl; R 2 - carbamoylaminoalkyl, mono-di-alkylcarbamoy-1-alkylalkyl, carbamoylaminoalkoxyl, m- and di-alkylcarbamoylaminoalkoxy, carbamoyloxyalkyl, mono- and di-alkylcarbamoyloxyalkylalkylalkylalkylalkylalkylalkylalkylalkylalkylalkyl 3 carbon atoms; R 3 is hydrogen, halogen, or their salts, characterized in that the compound of the general formula OCH ^ SNONCH g NH 2 where R 2 · and R 3 have the indicated meanings, are reacted with a compound of the general formula ZR z , where R has the indicated meanings, and Z is the reactive esterified esterified hydroxyl group, followed by isolation of the desired product in free form or in the form of salt.
类似技术:
公开号 | 公开日 | 专利标题 SU841581A3|1981-06-23|Method of preparing derivatives of alkanolamine or their salts GB1467061A|1977-03-16|Quinolines and process for their manufacture IE41528L|1975-04-27|Furfuryl-benzomorphane derivatives. ES8301990A1|1983-01-01|2-Carbamimidoyl-6-substituted-1-carbadethiapen-2-em-3-carboxylic acids, a process for preparing and an antibiotic composition comprising the same. GB1428793A|1976-03-17|Cephalosporins WO1999020639A3|1999-07-08|NOVEL 3,6-HEMIKETALS FROM THE CLASS OF 9a-AZALIDES SE447118B|1986-10-27|4 "-DEOXI-4" ACYLAMIDO DERIVATIVES OF OLEANDOMYCINES, ERYTHROMYCINES AND ERYTHROMYCINE CARBONATE KR960017649A|1996-06-17|Aminocyclopentane derivatives GB1314830A|1973-04-26|Pharmaceutically useful benzomorphanes and their production ES437009A1|1977-04-01|Benzylpyrimidine derivatives SU1020004A3|1983-05-23|Process for preparing derivatives of oleandomycin GB1212174A|1970-11-11|Process for the production of new 2-oxo-1,2-dihydroquinoline derivatives GB1464431A|1977-02-16|Indolobenzazepine derivatives and a process for the manufacture thereof IE40676B1|1979-08-01|Derivatives of 5-hydroxy-2,3-dihydro-1h-dibenzo-| thiepino and oxepino-| pyrrole,methods for their preparation,and compositions containing them IE43117L|1976-12-16|Naphthacene derivatives KR950003300A|1995-02-16|New cephalosporin antibiotics and preparation method thereof RU2002124772A|2004-02-20|PLURAFLAVINS AND THEIR DERIVATIVES, METHOD FOR PRODUCING THEM AND THEIR USE IE771799L|1978-02-28|Cephalosporins. SE8302517L|1983-05-03|PROCEDURE FOR THE PREPARATION OF ANTIBIOTIC C-15003 P-0 | FR2331335B2|1979-05-25| ES441965A1|1977-08-01|Acyl derivatives of clavulanic acid methods for their preparation and compositions containing them IE47968B1|1984-08-08|Oleandomycin-derived carbamates and thiocarbamates US4973693A|1990-11-27|Novel pentacyclic compound and stereoselective synthesis thereof FR2383161A1|1978-10-06|PROCESS FOR PREPARING NEW N-ALCOYL DERIVATIVES OF 1-PHENYL-2-AMINO-1,3-PROPANEDIOL, COMPOUNDS OBTAINED BY THIS PROCESS AND MEDICINAL PRODUCTS CONTAINING THE SAID COMPOUNDS FR2452495A1|1980-10-24|2-EPI-FORTIMICINS A AND B AND DERIVATIVES THEREOF, ESPECIALLY USEFUL AS ANTIBIOTICS, AND INTERMEDIATES FOR THEIR PREPARATION
同族专利:
公开号 | 公开日 IE38060L|1974-01-06| CH599136A5|1978-05-12| AR206214A1|1976-07-07| IE38060B1|1977-12-21| ES440954A1|1977-07-01| US3930016A|1975-12-30| DK137234C|1978-07-10| AU5758473A|1975-01-09| FI63745C|1983-08-10| ZA733757B|1974-08-28| CH598205A5|1978-04-28| HK53679A|1979-08-10| MY8000088A|1980-12-31| CH605698A5|1978-10-13| FR2191899B1|1977-08-19| FR2191899A1|1974-02-08| DE2332837A1|1974-01-24| CA1088557A|1980-10-28| SE386892B|1976-08-23| ES440955A1|1977-07-01| NL7309473A|1974-01-08| DE2332837C2|1982-04-08| ATA588973A|1976-08-15| JPS5630342B2|1981-07-14| DK137234B|1978-02-06| AR205611A1|1976-05-21| FI63745B|1983-04-29| IT7950873D0|1979-11-21| AT347475B|1978-12-27| ES416605A1|1976-06-16| JPS54117437A|1979-09-12| NO142033B|1980-03-10| SU559642A3|1977-05-25| JPS4951232A|1974-05-18| GB1436173A|1976-05-19| NO142033C|1980-06-18| BE801650A|1973-10-15| JPS5544740B2|1980-11-13|
引用文献:
公开号 | 申请日 | 公开日 | 申请人 | 专利标题 NL301580A|1962-12-11| US3466325A|1965-04-30|1969-09-09|Haessle Ab|1- - 2-hydroxy-3-isopropylaminopropanes and the salts thereof| GB1199037A|1967-09-27|1970-07-15|Ici Ltd|Alkanolamine Derivatives| SE372762B|1969-05-21|1975-01-13|Haessle Ab|US4038313A|1970-01-08|1977-07-26|Ciba-Geigy Corporation|Cycloalkylureido phenoxy propanolamines| AT334385B|1973-12-20|1976-01-10|Chemie Linz Ag|PROCESS FOR THE PREPARATION OF NEW PHENOXYPROPYLAMINE DERIVATIVES AND THEIR SALTS| SE7402096L|1974-02-18|1975-08-19|United Aircraft Corp| US4145363A|1975-02-05|1979-03-20|Yamanouchi Pharmaceutical Co., Ltd.|4-Carbamoylamino-α-aminomethylbenzyl alcohol derivatives| DE2645710C2|1976-10-09|1985-06-27|Merck Patent Gmbh, 6100 Darmstadt|Phenoxy-aminopropanols, process for their manufacture and pharmaceutical preparation| US4219561A|1977-09-22|1980-08-26|Imperial Chemical Industries Limited|Alkanolamine derivatives| US4243681B1|1977-10-11|1985-09-10| US4147805A|1978-07-28|1979-04-03|Mead Johnson & Company|Alkylthiophenoxyalkylamines and the pharmaceutical use thereof| IT1147311B|1980-02-13|1986-11-19|Stabil Bioterapico Farmachim|BASIC ETHERS OF 4-HYDROXY-BENZOFENONES WITH ACTIVITIES SUCH AS BETABLOCCANT AGENTS AND RELATED PREPARATION PROCEDURE| SE8004088L|1980-06-02|1981-12-03|Haessle Ab|NEW SUBSTITUTED 3-PHENOXI-L-ALCOXICARBONYLALKYLAMINO-PROPANOL-2 WITH BETA-RECEPTOR BLOCKING PROPERTIES AND PROCEDURE FOR THEIR PREPARATION, PHARMACEUTICAL PREPARATIONS OF THE METHOD| JPS6313427B2|1981-08-20|1988-03-25|Mitsubishi Chem Ind| US4470965A|1982-10-27|1984-09-11|Usv Pharmaceutical Corporation|Celiprolol for the treatment of glaucoma| US4665094A|1985-08-29|1987-05-12|Merck & Co., Inc.|Oculoselective beta-blockers for treatment of elevated intraocular pressure| US4945182A|1985-12-24|1990-07-31|Merck & Co., Inc.|Oculoselective beta-blockers| EP0252007A3|1986-06-28|1989-07-05|Ciba-Geigy Ag|2-propanol derivatives as corrosion inhibitors| SE8801518D0|1988-04-22|1988-04-22|Astra Pharma Prod|A NOVEL PROCESS|
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申请号 | 申请日 | 专利标题 SE7208927A|SE386892B|1972-07-06|1972-07-06|PROCEDURE FOR THE PREPARATION OF OXAMINO COMPOUNDS| 相关专利
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