CS210993B1 - Preparation method of 1,2,3,4,5,6-hexahydro-1-benzazotin - Google Patents

Preparation method of 1,2,3,4,5,6-hexahydro-1-benzazotin Download PDF

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Publication number
CS210993B1
CS210993B1 CS928579A CS928579A CS210993B1 CS 210993 B1 CS210993 B1 CS 210993B1 CS 928579 A CS928579 A CS 928579A CS 928579 A CS928579 A CS 928579A CS 210993 B1 CS210993 B1 CS 210993B1
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CS
Czechoslovakia
Prior art keywords
hexahydro
preparation
toluene
benzazotin
aluminum hydride
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Application number
CS928579A
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Czech (cs)
Slovak (sk)
Inventor
Jan Jedrichovsky
Alfonz Rybar
Richard Frimm
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Jan Jedrichovsky
Alfonz Rybar
Richard Frimm
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Application filed by Jan Jedrichovsky, Alfonz Rybar, Richard Frimm filed Critical Jan Jedrichovsky
Priority to CS928579A priority Critical patent/CS210993B1/en
Publication of CS210993B1 publication Critical patent/CS210993B1/en

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Description

Postupom podlá vynálezu sa předmětná -tetrahydro-1-benzazocín-2/1H/-onu vzorca zlúčenina vzorca I získává redukciou 3,4,5,6IIAccording to the process of the invention, the subject -tetrahydro-1-benzazocin-2 (1H) -one of formula (I) is obtained by reduction of 3,4,5,6II

H z?H z?

N—<N— <

/11/ komplexnými a1 umíniumhydr ídmi. Redukci a sa prevádza di-/alkoxy/nátr iumaluminiumhydridmi obecného vzorca III(11) with complex aluminium hydrides. The reduction a is carried out with di- (alkoxy) sodium aluminum hydrides of the formula III

NaAlH2[0/CH2/n0R 2] kde n x 1 až 5 a R je popřípadě rozvětvený alkyl C^-C^, v aromatickom rozpúštadle za varu.NaAlH 2 [O / CH 2 / n OR 2 ] wherein n x 1 to 5 and R is an optionally branched C 1 -C 4 alkyl, in the aromatic solvent at boiling.

Výhodou postupu podlá vynálezu je omnoho vyššia bezpečnost práce, kratsia reakčná doba /6 hod/a vyššie výtažky /80 až 90 %/ oproti dosial používanej metóde. Ďalšou výhodou je používanie tuzemského přípravku di-/raetoxyetoxy/-nátriumalumíniumhydridu proti dovázanému 1 itiumalumíniurahydridu.Advantages of the process according to the invention are much higher work safety, shorter reaction time (6 hours) and higher yields (80 to 90%) compared to the method used up to now. Another advantage is the use of a domestic preparation of di- (methoxyethoxyethoxy) sodium aluminum hydride over imported lithium aluminum hydride.

V dalsom je predmet vynálezu objasněný na příklade bez toho, aby sa na tento výlučné obmedzoval:In the following, the subject matter of the invention is illustrated by way of example without limiting this:

K zmesi 2,75 1 70% roztoku di-/metoxyetocy/nátriuraalumíniumhydridu v toluéne a 2,75 1 bezv. toluénu sa za miešania prikvapká roztok 0,875 kg 3,4,5,6-1 e t r ahyd ro - 1-benzaz-oc ínu-2/lH/-onu v 10 1 bezv. toluénu tak, aby roztok rovnoměrně vřel.To a mixture of 2.75 L of a 70% solution of di- / methoxyetocyte / sodium aluminum hydride in toluene and 2.75 L of aq. of toluene is added dropwise with stirring a solution of 0.875 kg of 3,4,5,6-1-tetrahydro-1-benzazoline-2 (1H) -one in 10 l of anhydrous toluene. toluene so that the solution boils evenly.

Po přidaní sa zmes refluxuje ešte 6 hodin. Po schladeni sa pomaly za miešania přidá 5 1 30% roztoku hydroxidu sodného. Toluénová vrstva sa oddělí a vodná extrahuje 3 1 toluénu. Spojené toluénové vrstvy sa premyjú vodou a vysušia bezv. síranom sodným. Po oddestilovaní toluénu sa zvyšok destiluje vákuovo. Získá sa 0,7 kg /88 %/ 1,2,3,4,5,6-hexahydro-1-benzazocínu t. v. 112 °C/1,33 kPa.After the addition, the mixture was refluxed for a further 6 hours. After cooling, 5 L of a 30% sodium hydroxide solution was added slowly with stirring. The toluene layer was separated and the aqueous extracted with 3 L of toluene. The combined toluene layers were washed with water and dried over anhydrous. sodium sulfate. After toluene was distilled off, the residue was distilled in vacuo. 0.7 kg (88%) of 1,2,3,4,5,6-hexahydro-1-benzazocine is obtained, m.p.

Claims (1)

PREDMET VYNÁLEZUOBJECT OF THE INVENTION Spósob přípravy 1,2,3,4,5,6-hexahydro-1-benzazocínu vzorca IA process for the preparation of 1,2,3,4,5,6-hexahydro-1-benzazocine of formula I HH ΛΜredukciou 3,4,5,6-tetrahydro-1-benzazocín-2i 1H/-ónu vzorca IX /1/ /11/Reduction of 3,4,5,6-tetrahydro-1-benzazocin-2H-1-one of formula IX (1) (11) H 0 komplexnými alumíniumhydridami, vyznačujúci sa tým, že sa redukcia prevádza di-/alkoxy/nátriumalumíniumhydridora obecného vzorca IIIH 2 is a complex aluminum hydride, characterized in that the reduction is carried out by a di- / alkoxy / sodium aluminum hydride of the formula III NaAm2[0/CH2/nOR 2J /111/ kde n = 1 až 5 a R je popřípadě rozvětvený alkyl C^-C^, v prostředí aromatického rozpúŠtadla za varu.NaAm 2 [O (CH 2 ) n OR 2 ] (111) wherein n = 1 to 5 and R is optionally branched C 1 -C 4 alkyl, in the presence of an aromatic solvent at boiling.
CS928579A 1979-12-22 1979-12-22 Preparation method of 1,2,3,4,5,6-hexahydro-1-benzazotin CS210993B1 (en)

Priority Applications (1)

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CS928579A CS210993B1 (en) 1979-12-22 1979-12-22 Preparation method of 1,2,3,4,5,6-hexahydro-1-benzazotin

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Application Number Priority Date Filing Date Title
CS928579A CS210993B1 (en) 1979-12-22 1979-12-22 Preparation method of 1,2,3,4,5,6-hexahydro-1-benzazotin

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CS210993B1 true CS210993B1 (en) 1982-01-29

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