Method of preparing phenethanolamine derivatives, free, in form of salt, racemate or optically activ

专利摘要:
Compounds of the formula (IV) <CHEM> wherein: R2 is methyl or ethyl R3 is hydroxy, C1-C4 alkanoyloxy, aminocarbonyl, methylaminocarbonyl or C1-C2 alkoxycarboxyl; and @@ is an asymmetric carbon atom having the S absolute stereochemical configuration. The compounds are useful intermediates in the preparation of phenethanolamines having pharmaceutical properties.
公开号:SU849997A3
申请号:SU792782302
申请日:1979-07-02
公开日:1981-07-23
发明作者:Миллз Джек；Курт Шмайгель Клаус；Норман Вальтер
申请人:Эли Лилли Энд Компани (Фирма)；
IPC主号:

专利说明:

(54) METHOD FOR PRODUCING FBNETHANOLAMINE DERIVATIVES IN FREE FORM, IN SALT, RACEEM OR OPTICALLY ACTIVE ANTIPOD
The invention relates to methods for the preparation of phenetano amine derivatives with high pharmacological activity and ALWAYS. HSCI agents that reduce or prevent the formation of adipose tissue in mpekopitakvdih, and this is still unknown, their activity in compounds of this type is accompanied by minimal side effects. influences. Various alkanolamine derivatives are known, possessing B-adrenergic blocking activity, in particular, a method for preparing phenethanolamine form derivatives, RNA CHOH-CH -NH-CHj-CHj 5 5 mules, where R is a halogen or hydroxy group, which means that the haloaceto 4) The enone of the formula CO-saHa-X, where X is chlorine or bromine, is reacted with dipheyl-3, 3-propylamine fl. There is also known a process for the preparation of m-substituted phenoxyethylamines of the formula fyo (CHa) "- NHR where R," 2 alkyl, consisting in the reaction of a compound of the formula O-CHjA, where A is AA-CH-CH4, with the corresponding amine. The purpose of the invention is to expand the range of products acting on a living organism. The goal is achieved by the fact that the derivatives of phenethanolamine of the formula BncNlMHCN -sNCHz R

权利要求:
Claims (1)
[1]
Claim
A method of obtaining derivatives of phenethanolamine of the formula I where
Rj is hydrogen or fluorine;
R.- aminocarbonyl, methylamino ’carbonyl or C ^ - C ^ -alkoxycarbonyl.
their salts, about t th h styrene oxide or the fact that / ° X
CH-CH _g> a nd a nd formula where R has the indicated interaction with the corresponding derivatives of propylamine of the formula, sub-. Followed by the introduction of the target product in the form of a free compound, salt, racemate or optically active antipodes.

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引用文献:

---

公开号 | 申请日 | 公开日 | 申请人 | 专利标题

---

---

NL56308C|1941-03-15|

---

GB1200886A|1966-09-23|1970-08-05|Allen & Hanburys Ltd|Phenylaminoethanol derivatives|

---

GB1301134A|1970-07-18|1972-12-29|Pfizer Ltd|SUBSTITUTED 1-PHENYL-2-ALLYLAMINO-ALKANOLS, 1-PHENYL-2-ALLYLAMINO-ALKANES AND alpha-AMINOALKYLPHENYL KETONES|

---

BE788850A|1972-09-15|1973-03-15|Hoffmann La Roche|BENZOIC ACID DERIVATIVES|

---

US4000192A|1973-05-07|1976-12-28|Allen & Hanburys Limited|Pharmacologically active compounds|

---

IE39247B1|1973-05-07|1978-08-30|Allen & Hanburys Ltd|Substituted benzamides|

---

NZ190854A|1978-06-28|1984-10-19|Beecham Group Ltd|2-hydroxy-2-phenyl ethylamine derivatives;pharmaceutical compositions|

---

CA1145766A|1978-07-03|1983-05-03|Jack Mills|Optically active phenethanolamines and methodfor increasing cardiac contractility|EP0006735B1|1978-06-28|1983-06-15|Beecham Group Plc|Secondary amines, their preparation, pharmaceutical compositions containing them and their use|

---

AT2265T|1979-10-25|1983-02-15|Beecham Group Plc|SECOND AMINE, THEIR PRODUCTION AND USE IN PHARMACEUTICAL COMPOSITIONS.|

---

EP0029320B1|1979-11-15|1985-07-10|Beecham Group Plc|Secondary ethanol amines, their preparation and their use in pharmaceutical compositions|

---

EP0040000B1|1980-05-08|1983-10-12|Beecham Group Plc|Arylethanolamine derivatives, their preparation and use in pharmaceutical compositions|

---

EP0066351B1|1981-03-06|1985-06-26|Beecham Group Plc|Arylethanol amine derivatives, their preparation and use in pharmaceutical compositions|

---

EP0061907B1|1981-03-31|1984-08-01|Beecham Group Plc|Secondary amines, their preparation, pharmaceutical compositions containing them and their use|

---

EP0070133B1|1981-07-11|1986-05-14|Beecham Group Plc|Secondary phenylethanol amines, processes for their preparation and their pharmaceutical application|

---

EP0089154A3|1982-03-12|1984-08-08|Beecham Group Plc|Ethanolamine derivatives, their preparation and use in pharmaceutical compositions|

---

CA1219865A|1982-05-14|1987-03-31|Leo Alig|Aziridine phenethanolamine derivatives|

---

CA1258454A|1982-08-10|1989-08-15|Leo Alig|Phenethanolamines|

---

IL69788A|1982-09-27|1987-01-30|Lilly Co Eli|Process for preparing 2-hydroxy-2-phenylethylamines,and novel silylated intermediates therefor|

---

EP0204948B1|1983-01-31|1990-03-28|Eli Lilly And Company|Growth promotion of animals with phenethanol amines|

---

US5166218A|1983-10-19|1992-11-24|Hoffmann-La Roche Inc.|Phenoxypropanolamines and pharmaceutical compositions thereof|

---

CA1262729A|1983-10-19|1989-11-07|Leo Alig|Phenoxypropanolamines|

---

US4602044A|1983-12-19|1986-07-22|Eli Lilly And Company|β-phenethanolamine antiobesity agents|

---

EP0151513A1|1984-01-12|1985-08-14|Eli Lilly And Company|Inotropic agent|

---

GB8505284D0|1985-03-01|1985-04-03|Beecham Group Plc|Growth promoters|

---

ES8800842A1|1985-03-01|1987-12-01|Beecham Group Plc|Ethanolamine derivatives for administering to livestock.|

---

IT1204416B|1986-06-27|1989-03-01|Midy Spa|PHENYLETHANOLAMINE ANALOGUE-BASED DRUGS FOR THE TREATMENT OF GASTRO-INTESTINAL AND UTERINE DISORDERS|

---

JP2837408B2|1987-05-30|1998-12-16|鐘紡株式会社|Acrylic fiber treatment method|

---

US5135955A|1988-04-25|1992-08-04|Eli Lilly And Company|Propanamine derivatives|

---

FI892341A|1988-06-10|1989-12-11|Hoffmann La Roche|PROPANOLAMINDERIVAT.|

---

CA2023954C|1989-10-17|1999-05-04|Hiroyuki Nohira|Process for the optical resolution of 2- phenylpropionic acid|

---

US6313146B1|1991-08-23|2001-11-06|Nps Pharmaceuticals, Inc.|Calcium receptor-active molecules|

---

KR100251995B1|1991-08-23|2000-06-01|젠센 제임스 유.|Calcium receptor active molecules|

---

US5763569A|1991-08-23|1998-06-09|The Brigham And Women's Hospital, Inc|Calcium receptor-active molecules|

---

US6011068A|1991-08-23|2000-01-04|Nps Pharmaceuticals, Inc.|Calcium receptor-active molecules|

---

US5962314A|1993-02-23|1999-10-05|Nps Pharmaceuticals, Inc.|Calcium receptor-active molecules|

---

US5688938A|1991-08-23|1997-11-18|The Brigham & Women's Hospital, Inc.|Calcium receptor-active molecules|

---

DE122005000033I1|1994-10-21|2005-09-29|Nps Pharma Inc|Calcium receptor active compounds.|

---

US6031003A|1991-08-23|2000-02-29|Nps Pharmaceuticals, Inc.|Calcium receptor-active molecules|

---

US6001884A|1991-08-23|1999-12-14|Nps Pharmaceuticals, Inc.|Calcium receptor-active molecules|

---

US5858684A|1991-08-23|1999-01-12|The Brigham And Women's Hospital, Inc.|Method of screening calcium receptor-active molecules|

---

US5321036A|1993-02-10|1994-06-14|Bristol-Myers Squibb Company|Thiazole and oxazole-based β3 adrenergic receptor agonists|

---

DK0907631T3|1996-05-01|2003-09-22|Nps Pharma Inc|Inorganic ion receptor active compounds|

---

US7321065B2|2003-04-18|2008-01-22|The Regents Of The University Of California|Thyronamine derivatives and analogs and methods of use thereof|

法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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US92167078A| true| 1978-07-03|1978-07-03|

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