[go: up one dir, main page]

NO171106B - PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL - Google Patents

PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL Download PDF

Info

Publication number
NO171106B
NO171106B NO900651A NO900651A NO171106B NO 171106 B NO171106 B NO 171106B NO 900651 A NO900651 A NO 900651A NO 900651 A NO900651 A NO 900651A NO 171106 B NO171106 B NO 171106B
Authority
NO
Norway
Prior art keywords
benzyl
tetralone
naphthol
mol
benzaldehyde
Prior art date
Application number
NO900651A
Other languages
Norwegian (no)
Other versions
NO900651D0 (en
NO171106C (en
NO900651L (en
Inventor
Douglas Guy Batt
Original Assignee
Du Pont Merck Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US06/839,912 external-priority patent/US4833164A/en
Publication of NO900651L publication Critical patent/NO900651L/en
Application filed by Du Pont Merck Pharma filed Critical Du Pont Merck Pharma
Priority to NO900651A priority Critical patent/NO171106C/en
Publication of NO900651D0 publication Critical patent/NO900651D0/en
Publication of NO171106B publication Critical patent/NO171106B/en
Publication of NO171106C publication Critical patent/NO171106C/en

Links

Landscapes

  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Foreliggende oppfinnelse angår en ny fremgangsmåte for fremstilling av 2-benzyl-l-nafthol av formel. Ved fremgangsmåten ifølge foreliggende oppfinnelse behandles en blanding av benzaldehyd og alfa-tetralon i t-butanol med kalium-t-butoxyd.The present invention relates to a novel process for the preparation of 2-benzyl-1-naphthol of formula. In the process of the present invention, a mixture of benzaldehyde and alpha-tetralone in t-butanol is treated with potassium t-butoxide.

Description

Foreliggende oppfinnelse angår en fremgangsmåte for fremstilling av 2-benzyl-l-nafthol. The present invention relates to a method for the production of 2-benzyl-1-naphthol.

Kjent teknikk Known technique

Et utall publikasjoner beskriver 2-alkyl-l-naftholer som mellomprodukter ved fremstilling av andre kjemiske for-bindelser, innbefattende N.S. Narasimhan og R.S. Mali, Tetrahedron, 31, 1005 (1975); Newman et al., J. Org. Chem., 43, 524 (1978); B. Miller og W. Lin, J. Org. Chem., .43, 4441 A number of publications describe 2-alkyl-1-naphthols as intermediates in the preparation of other chemical compounds, including N.S. Narasimhan and R.S. Mali, Tetrahedron, 31, 1005 (1975); Newman et al., J. Org. Chem., 43, 524 (1978); B. Miller and W. Lin, J. Org. Chem., .43, 4441

(1978); K.A. Parker og J.L. Kallmerton, Tetrahedron Letters, 14, 1197 (1979); D.W. Cameron et al., Aust J. Chem, 35, 1481 (1978); K. A. Parker and J.L. Kallmerton, Tetrahedron Letters, 14, 1197 (1979); D.W. Cameron et al., Aust J. Chem, 35, 1481

(1982); P. Barua et al., Chem. Ind., 303, (1984); T. (1982); P. Barua et al., Chem. Ind., 303, (1984); T.

Kometani et al., J. Org. Chem., 48, 2630 (1983); T. Zhong og M. Huang, Hua Hseuh Hseuh Pao, 39, 229 (1981); C. Pac et Kometani et al., J. Org. Chem., 48, 2630 (1983); T. Zhong and M. Huang, Hua Hseuh Hseuh Pao, 39, 229 (1981); C. Pac et

al., Synthesis, 589 (1978); I.A. Akhtar og J.J. McCullough i J. Org. Chem., 4_6, 1447 (1981); R. Alonso Cermona et al., al., Synthesis, 589 (1978); I.A. Akhtar and J.J. McCullough in J. Org. Chem., 4-6, 1447 (1981); R. Alonso Cermona et al.,

An. Quim., Ser. C., 78, 9 (1982); I.M. Andreeva et al., An. Quim., Ser. C., 78, 9 (1982); I. M. Andreeva et al.,

Khim. Geterotsikl. Soedin., 2, 181 (1983); D. Berney og Kr Schuh, Heiv. Chim. Acta, 62, 1268 (1979); S.P. Starkov, Izv. Vyssh. Uchebn. Zaved., Khim. Khim Tekhnol., 20, 1099 (1977); M.R. Saidi, Indian J. Chem., 474 (1982); L.Z. Oblasova og G.D. Kharlampovich, Khim. Pro-St. (Moscow), 10, 776 (1977); F.T. Sher og G.A. Berchtold, J. Org. Chem., 42, 2569 (1977); M. Mully et al., Heiv. Chim. Acta, 58, 610 (1975); T.R. Kasturi og R. Sivaramakrishnan, Proe. Indian Acad. Sei., 86, 309 (1977) og T. Hirashima et al. i japansk patent nr. 7010339, bevilget 14. april 1970. Kim. Goat root cycle. Soedin., 2, 181 (1983); D. Berney and Kr Schuh, Heiv. Chim. Acta, 62, 1268 (1979); S. P. Starkov, Izv. Vyssh. Uchebn. Zaved., Khim. Khim Technol., 20, 1099 (1977); M. R. Saidi, Indian J. Chem., 474 (1982); L.Z. Oblasova and G.D. Kharlampovich, Khim. Pro-St. (Moscow), 10, 776 (1977); F.T. Sher and G.A. Berchtold, J. Org. Chem., 42, 2569 (1977); M. Mully et al., Heiv. Chim. Acta, 58, 610 (1975); T.R. Kasturi and R. Sivaramakrishnan, Proe. Indian Acad. Sci., 86, 309 (1977) and T. Hirashima et al. in Japanese Patent No. 7010339, granted April 14, 1970.

Et utall publikasjoner beskriver 2-benzyl-l-nafthol A number of publications describe 2-benzyl-1-naphthol

som en kjemisk gruppe, slik som B. Miller og W. Lin, J. Org. Chem., 44, 887 (1979) og Z. Aizenshtat et al., J. Org. as a chemical group, such as B. Miller and W. Lin, J. Org. Chem., 44, 887 (1979) and Z. Aizenshtat et al., J. Org.

Chem., 42, 2386 (1977). Chem., 42, 2386 (1977).

Ifølge oppfinnelsen er det tilveiebrakt en fremgangsmåte for fremstilling av 2-benzyl-l-nafthol av formel: According to the invention, a method has been provided for the production of 2-benzyl-1-naphthol of the formula:

hvori det som utgangsmateriale anvendes tetralon og benzaldehyd, kjennetegnet ved at en blanding av benzaldehyd og alfa-tetralon i t-butanol behandles med kaliumbutoxyd. in which tetralone and benzaldehyde are used as starting materials, characterized in that a mixture of benzaldehyde and alpha-tetralone in t-butanol is treated with potassium butoxide.

Fremgangsmåten ifølge den ovenfor refererte publikasjon av Miller et al. beskriver en omleiring av nafthalenoner i syre. Alt denne synes å gjøre er å forskyve carbonylgruppen eller frembringe en ny carbonylgruppe som kan derivatiseres videre. The method according to the above-referenced publication by Miller et al. describes a rearrangement of naphthalenones in acid. All this seems to do is displace the carbonyl group or produce a new carbonyl group which can be derivatized further.

Den refererte publikasjon av Aizenshtat et al. angir i første avsnitt at de nå eksisterende (1976) synteser er fremgangsmåter som er ineffektive og som gir lave utbytter. På side 2388 beskriver Aizenshtat fremstilling av 2-benzyl-l-naf thol ved isoaromatisering, som vist i 8-10 og i figur 2. Som det fremgår er katalysatorsystemet og løsningsmiddel systemet temmelig kompleks og, som vist under figur 2, har difenylether et kokepunkt ved 255 °C. The referenced publication by Aizenshtat et al. states in the first paragraph that the now existing (1976) syntheses are procedures which are inefficient and which give low yields. On page 2388, Aizenshtat describes the preparation of 2-benzyl-l-naphthol by isoaromatization, as shown in 8-10 and in figure 2. As can be seen, the catalyst system and solvent system are rather complex and, as shown under figure 2, diphenyl ether has a boiling point at 255 °C.

Fremgangsmåten ifølge foreliggende oppfinnelse anvender i forhold enkle reaksjonsmediematerialer, mindre strenge betingelser og starter direkte med tetralon og benzaldehyd uten å gå via benzylidén. The method according to the present invention uses relatively simple reaction medium materials, less stringent conditions and starts directly with tetralone and benzaldehyde without going via the benzylidene.

Den angitte referanse av Barton et al. viser på s. 16 i beskrivelsen at 2-benzyl-l-nafthol fremstilles ved isomeri-sering av et benzyliden-tetralon med en rhodium-katalysator i etanolkloroform. The cited reference by Barton et al. shows on p. 16 of the description that 2-benzyl-1-naphthol is produced by isomerization of a benzylidene tetralone with a rhodium catalyst in ethanol chloroform.

Kjent teknikk viser ved disse referanser en reaksjonsrekke som går fra tetralon til en intermediær forbindelse og deretter til 2-benzyl-l-nafthol. Fremgangsmåten ifølge foreliggende oppfinnelse går fra et tetralon direkte til 2-benzyl-l-nafthol uten å gå gjennom en særskilt intermediær forbindelse, ved at reaksjonen utføres i t-butanol med t-butoxyd. Dette er nytt; det sparer et fremgangsmåtetrinn og anvender enkle materialer og ikke fremmedartede katalysatorer som anvendt i fremgangsmåten ifølge de refererte publikasjoner . Known technology shows in these references a reaction series that goes from tetralone to an intermediate compound and then to 2-benzyl-1-naphthol. The method according to the present invention goes from a tetralone directly to 2-benzyl-1-naphthol without going through a special intermediate compound, by the reaction being carried out in t-butanol with t-butoxide. This is new; it saves a method step and uses simple materials and not foreign catalysts as used in the method according to the referenced publications.

Ved anvendelse av fremgangsmåten ifølge foreliggende oppfinnelse fremstilles 2-benzyl-l-nafthol analogt med det nedenfor beskrevne utførelseseksempel for fremstilling av 2-(2-hydroxyfenylmethyl)-l-nafthol. When using the method according to the present invention, 2-benzyl-1-naphthol is produced analogously to the embodiment described below for the production of 2-(2-hydroxyphenylmethyl)-1-naphthol.

Claims (1)

Fremstillinqseksempel: 2-( 2- hydroxyfenylmethyl)- l- naftholProduction example: 2-(2-hydroxyphenylmethyl)-1-naphthol En løsning av 5,85 g (0,040 mol) 1-tetralon og 4,88 g (0,40 mol) salicylaldehyd i 400 ml t-butanol ble behandlet med 17,6 g (0,160 mol) kalium t-butoxyd og ble oppvarmet til til-bakeløpskoking i 16 timer. Etter avkjøling til romtemperatur ble løsningen helt over i omrørt 1,0 N saltsyre. Etter iso-lering ved ekstraksjon med ethylacetat ble det urene produkt kromatografert med 4:1 petroleumether/ether under dannelse av et brunt, fast materiale. Dette ble omkrystallisert (cyclo-hexan/kloroform) under dannelse av 5,24 g (52 %) av tittelfor-bindelsen som hvite nåler med sm.p. 124-125 °.A solution of 5.85 g (0.040 mol) of 1-tetralone and 4.88 g (0.40 mol) of salicylaldehyde in 400 ml of t-butanol was treated with 17.6 g (0.160 mol) of potassium t-butoxide and was heated to reflux for 16 hours. After cooling to room temperature, the solution was poured into stirred 1.0 N hydrochloric acid. After isolation by extraction with ethyl acetate, the crude product was chromatographed with 4:1 petroleum ether/ether to give a brown solid. This was recrystallized (cyclohexane/chloroform) to give 5.24 g (52%) of the title compound as white needles, m.p. 124-125 °. Fremgangsmåte for fremstilling av 2-benzyl-l-nafthol av formel: hvori det som utgangsmateriale anvendes tetralon og benzaldehyd,karakterisert ved at en blanding av benzaldehyd og alfa-tetralon i t-butanol behandles med kaliumbutoxyd.Process for the production of 2-benzyl-l-naphthol of formula: in which tetralone and benzaldehyde are used as starting materials, characterized in that a mixture of benzaldehyde and alpha-tetralone in t-butanol is treated with potassium butoxide.
NO900651A 1985-05-08 1990-02-09 PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL NO171106C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
NO900651A NO171106C (en) 1985-05-08 1990-02-09 PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US73179185A 1985-05-08 1985-05-08
US06/839,912 US4833164A (en) 1985-05-08 1986-03-19 2-substituted-1-naphthols, pharmaceutical compositions of, and their use as 5-lipoxygenase inhibitors
NO861829A NO164592C (en) 1985-05-08 1986-05-07 PROCEDURE FOR THE PREPARATION OF 2-SUBSTITUTED-1-NAFTHOLS.
NO900651A NO171106C (en) 1985-05-08 1990-02-09 PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL

Publications (4)

Publication Number Publication Date
NO900651L NO900651L (en) 1986-11-10
NO900651D0 NO900651D0 (en) 1990-02-09
NO171106B true NO171106B (en) 1992-10-19
NO171106C NO171106C (en) 1993-01-27

Family

ID=27484135

Family Applications (1)

Application Number Title Priority Date Filing Date
NO900651A NO171106C (en) 1985-05-08 1990-02-09 PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL

Country Status (1)

Country Link
NO (1) NO171106C (en)

Also Published As

Publication number Publication date
NO900651D0 (en) 1990-02-09
NO171106C (en) 1993-01-27
NO900651L (en) 1986-11-10

Similar Documents

Publication Publication Date Title
Micheli et al. Total syntheses of optically active 19-nor steroids.(+)-Estr-4-ene-3, 17-dione and (+)-13. beta.-ethylgon-4-ene-3, 17-dione
Büchi et al. Terpenes. XVI. 1, 2 constitution of patchouli alcohol and absolute configuration of cedrene
Smissman et al. The Synthesis of 3-Alkoxy-cis-2-trans-4-unsaturated Acids1
Taber et al. Construction of the tricyclic ABC core of the Veratrum alkaloids
Herr et al. Synthesis of potent oral anabolic-androgenic steroids
Mazzola et al. 9H-Pyrrolo [1, 2-a] indoles
NO171106B (en) PROCEDURE FOR THE PREPARATION OF 2-BENZYL-1-NAFTHOL
Kende et al. Total synthesis of tetracyclines. IV. Synthesis of an anhydrotetracycline derivative
Bindra et al. An efficient route to intermediates for the synthesis of 11-deoxyprostaglandins
Snitman et al. Total synthesis of (.+-.)-ferruginol and (.+-.)-hinokione
Marchand et al. Syntheses of pentacyclo [5.4. 0.02, 6.03, 10.05, 9] undecane-4, 8, 11-trione, pentacyclo [6.3. 0.02, 6.03, 10.05, 9] undecane-4, 7, 11-trione (D3-trishomocubanetrione), and 4, 4, 7, 7, 11, 11-hexanitropentacyclo [6.3. 0.02, 6.03, 10.05, 9] undecane (D3-hexanitrotrishomocubane)
Fujii et al. Preparation of some ring-oxygenated phenacyl bromides
Edwards et al. Steroids. CCLXIII. 1 The Synthesis of 2-Formyl-Δ1-and-Δ1, 4-3-keto Steroids2
Hendrickson et al. a New Heterocycle Synthesis: Pyrroles and Quinolines
Marshall et al. Synthesis of Substituted cis-Cyclodecenes from Cyclooctanone
Moriconi et al. Ring Expansion of 2-Substituted 1-Indanones to 2-Hydroxyisocarbostyril Derivatives. Scope and Mechanism of Reaction. A Spectral Study of the Lactam—Lactim Tautomerism in Isocarbostyrils1
Walker Triton B in Synthesis of 3-Phenylcyclohexenones
Boekelheide et al. Coumarins as Intermediates in the Synthesis of Colchicine Analogs
Dentani et al. Cascade cyclization of 1, 2, 7, 8-tetraones and total synthesis of (±)-nesteretal A
Beard et al. 3-phenylcyclobutylamine. II
Moffett Central Nervous System Depressants. VIII. Pyroles.
Wasson et al. A synthesis of 6-hydroxy-1-benzoxepin-3, 5 (2H, 4H)-dione
KASHIHARA et al. Novel synthesis of indan derivatives
Wilt et al. Ring-Size Effects in the Neophyl Rearrangement. VI. 1 The 1-Phenylcycloheptylcarbinyl System
Baker et al. AN ANTIMALARIAL ALKALOID FROM HYDRANGEA. VII. 3-[β-KETO-γ-(5-HYDROXY-2-PIPERIDYL) PROPYL]-4-QUINAZOLONE, AN ISOMER

Legal Events

Date Code Title Description
MM1K Lapsed by not paying the annual fees

Free format text: LAPSED IN NOVEMBER 2002