CS200146B1 - N-/omega-phenoxyalkyl/piperidin-n-oxides and process for preparing thereof - Google Patents

N-/omega-phenoxyalkyl/piperidin-n-oxides and process for preparing thereof Download PDF

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CS200146B1
CS200146B1 CS36179A CS36179A CS200146B1 CS 200146 B1 CS200146 B1 CS 200146B1 CS 36179 A CS36179 A CS 36179A CS 36179 A CS36179 A CS 36179A CS 200146 B1 CS200146 B1 CS 200146B1
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Prior art keywords
phenoxyalkyl
oxides
piperidine
piperidin
omega
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CS36179A
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Czech (cs)
Slovak (sk)
Inventor
Ivan Lacko
Ferdinand Devinsky
Ludovit Krasnec
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Ivan Lacko
Ferdinand Devinsky
Ludovit Krasnec
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Application filed by Ivan Lacko, Ferdinand Devinsky, Ludovit Krasnec filed Critical Ivan Lacko
Priority to CS36179A priority Critical patent/CS200146B1/en
Publication of CS200146B1 publication Critical patent/CS200146B1/en

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Description

(54) N-(<n-fenoxyalkyl) piperidln-N-oxidy a sp&eob ich přípravy( 54 ) N - (<n -phenoxyalkyl) piperidine-N-oxides and methods for their preparation

Vynález sa týká. N-(cj-fenoxyalkyl)piperidín-N-oxidov obeeného vzorca.The invention relates. N- (C 1 -phenoxyalkyl) piperidine-N -oxides of the formula.

kde n značí 2 až 10, a sp&sobu ich přípravy. V súčasnosti majú asiínoxidy váaka niektorým svojim výhodným vlastnostiam široká využitie v priemysle. Používajú sa ako detergenčné, povrchovoaktívne látky, antioxidapty, dezinficienciá, kancerostatiká apod.. Zlúčeniny, ktoré sú podstatou vynálezu, aú nové, doteraz v literatúre neoplsané a zistili aa u nich doteraz neznáme účinky na niektoré kmene mikroorganizmev. Tento antimikrobiálny účinok bol vyšší alebo zrovnatelný s preparútmi typu améniových soli používanými v súčasnosti u nás.wherein n denotes 2 to 10, and a process for their preparation. Currently, some of its advantageous properties of vacuum asine oxides are widely used in industry. They are used as detergents, surfactants, antioxidants, disinfectants, carcinostatics and the like. The compounds of the present invention are novel and have not been disclosed in the literature yet and have found and yet unknown effects on certain microorganism strains. This antimicrobial effect was higher or comparable to the amenium salt formulations currently used in our country.

Ako je z literatúry známe, dajú sa amínoxidy pripraviť niekolkými spAsobmi /oxidáciou kyselinou Carovou, ozénom, hydrogénporoxidmi za katalýzy soli kovov, peroxidem vodíka apod./ Oxidácia má oproti iným sp&sobom přípravy amínoxidov tú výhodu, že vznikajú produkty vo vyaokom výtažku, vysokej čistoty, za použitia len malého množstva rozpúšťadla a reakčni doba je v porovnaní a inými metédami přípravy amínoxidov podstatné kratšia.As is known in the literature, amine oxides can be prepared in several ways / by oxidation with carboxylic acid, ozene, hydrogen peroxides under the catalysis of metal salts, hydrogen peroxide, etc./ Oxidation has the advantage over other methods of preparation of amine oxides using only a small amount of solvent and the reaction time is considerably shorter compared to other amine oxide preparation methods.

Nové zlúčeniny sa prlpravujú sp&sobom podía vynálezu, ktorého podstatou je, žo sa oxiduje příslušný terciárny amin N-(u>-fenoxýalkyl)piperidin 30 % vodným roztokom peroxidu vodíkav metanole pri teplote 60 °C počas 3 hodin.The novel compounds are prepared according to the invention by oxidizing the corresponding tertiary amine N- (n-phenoxyalkyl) piperidine with a 30% aqueous solution of hydrogen peroxide and methanol at 60 ° C for 3 hours.

200 146200 146

200 148200 148

Ka ilustráciu spdsobu přípravy ako i niektorých fyzikálnych konfitát sú uvedené následovně příklady.The following examples are given to illustrate the preparation method as well as some physical confitates.

Přiklad 1Example 1

V 20 mi metanolu sa rozpustí 0,1 mol N-(2-fenoxyetyl)piperidínu, zahřeje sa na 80 °C a pri tejto teplote ea přidá 0,12 mel 30% vodného roztoku peroxidu vodíka. Reakčná zmes sa nechá doreagovať ešte 3 hodiny. Po ochladeni, rozložení prebytočného peroxidu vodíka, odpa roní vody a 'rozpúšťadla sa surový produkt prekryStalizujo niekoíko krát do konfitantnej teploty topenia· Výťažok K-(2-fenoxyetyl)piperidín-N-oxidu je 79 %, t.t. 140 až 143 °C, elementárna analýza (vypočltané/nájderié 070,56/69,95, 08,65/8,89, 06,33/6,25, λ „ =219,270 nm.Dissolve 0.1 mol of N- (2-phenoxyethyl) piperidine in 20 ml of methanol, heat to 80 ° C and add 0.12 ml of a 30% aqueous hydrogen peroxide solution at this temperature e. The reaction mixture was allowed to react for a further 3 hours. After cooling, decomposition of excess hydrogen peroxide, evaporation of water and solvent, the crude product is recrystallized several times to a confident melting point. The yield of K- (2-phenoxyethyl) piperidine-N-oxide is 79%, m.p. 140-143 ° C, elemental analysis (calculated / found 070.56 / 69.95, 08.65 / 8.89, 06.33 / 6.25, λ "= 219.270 nm).

. na* ,. on* ,

Příklad 2Example 2

Pracovný postup je ten istý ako v přiklade 1, na oxidáeiu sa však použil K-(5-fenoxypentyl)piperidín. Výťažok produktu je 86 %, t.t. 166 až 169 °C, elementárna analýza (vypočítané/nájdené %): 072,97/72,64, 09,57/9,58, 05,32/5,09^^^221,271 nm.The procedure is the same as in Example 1, but K- (5-phenoxypentyl) piperidine was used for the oxidation. The product yield is 86%, m.p. 166-169 ° C, elemental analysis (calculated / found%): 072.97 / 72.64, 09.57 / 9.58, 05.32 / 5.09.

Příklad 3Example 3

Pracovný postup je ten istý ako v příklade 1, na oxidáeiu sa vfiak použil K-(8-fenoxyoktyl{piperidín. Výťažok produktu je 86 %, t.t. 117 až 120 °C, elementárna analýza (vypočl tané/nájdené %): 074,71/74,22, 010,23/9,98, 04,59/4,51, λ«220,271 nm.The procedure is the same as in Example 1 except that K- (8-phenoxyoctyl {piperidine) is used for the oxidation, yield 86%, mp 117-120 ° C, elemental analysis (calculated / found%): 074.71 (74.22, 010.23 / 9.98, 04.59 / 4.51, λ 220.271 nm).

Claims (2)

PREDMET VYNÁLEZUOBJECT OF THE INVENTION 1. N-(ůi-fenoxyalkyl) piperidín-N-oxidy obecného vzorca kde n značí 2 až 10.N - (1-phenoxyalkyl) piperidine-N-oxides of the formula wherein n is 2 to 10. 2* SpOsob přípravy zlúčenín podía bodu 1, vyznačujúci sa tým, že sana N-(6J-fenoxyalkyl)piperidíny obecného vzorca.2. A process for the preparation of the compounds according to claim 1, wherein the N- (6-phenoxyalkyl) piperidines are of the formula. kde n má ten istý význam ako v bode 1, pOsobí 30% vodným roztokom peroxidu vodíka pri teploto 60 °C počas3 hodin v prostředí metanolu.where n has the same meaning as in point 1, it is treated with a 30% aqueous hydrogen peroxide solution at 60 ° C for 3 hours in methanol.
CS36179A 1979-01-17 1979-01-17 N-/omega-phenoxyalkyl/piperidin-n-oxides and process for preparing thereof CS200146B1 (en)

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