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Process for the preparation of 2-alkyl cyclopent-2-enones

Assignee: Montedison SpA
•
Filing: 1986-03-03
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Granted: 1987-06-16
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Expires: 2006-03-03
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Abstract

Abstract A process for the preparation of 2-alkyl cyclopent-2-enones having the formula: ##STR1## wherein R is as defined hereinafter. An α-olefin having the formula CH 2 ═CH--CH 2 R is oxidized to the corresponding epoxide. The epoxide is reacted with an alkylating agent having the formula Na + [CH(COOR") 2 ] - , wherein R" is an ethyl, an isopropyl, or an isobutyl radical. An α-carbalkoxy-γ-alkyl lactone is obtained, which, through saponification and decarboxylation, yields a γ-alkyl lactone having the formula: ##STR2## which is reacted with a protic acid, thereby obtaining, by cyclization, the desired 2-alkylcyclopent-2-enone. The obtained products are intermediates for the production of pharmaceutical products and of drugs for veterinary use, in particular prostaglandin.

Inventors

  • 👤 Enrico Dalcanale

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 02:49
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/02; C07D307/26; C07D307/30; C07D307/32; C07D307/33; C07C; C07C255/00; C07C45/00; C07C45/56; C07C45/57; C07C45/59; C07C49/00; C07C49/587; C07C49/597; C07C49/687; C07C49/753; C07D303/00; C07D303/02; C07D303/38; C07D303/40; C07D303/42; C07D315/00

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 243 words
A process for the preparation of a 2-alkylcyclopenten-2-one having formula: where R is C n H 2n+1 (linear or branched); (CH 2 ) n --COOR'; (CH 2 ) n --NR' 2 ; (CH 2 ) n --OR'; (CH 2 ) n X or (CH 2 ) n --CN, n ranges from 1 to 20, X is Cl, Br, I or F, and R' is an alkyl group containing up to 5 carbon atoms, a benzyl group, or a phenyl group, the last two groups having optionally one or more substituent groups on the ring, wherein a saturated gamma-alkyl-lactone: ##STR21## is reacted at 20°-100° C. with a protic acid, thereby obtaining, by rearrangement, a 2-alkyl-cyclopenten-2-one (I), characterized in that said gamma-alkyl-lactone (V) is obtained through the following steps: (a) an epoxide: ##STR22## is made to react with an alkylating agent having the formula Na + [CH(COOR") 2 ] - (R" being an ethyl, isopropyl or isobutyl radical), in the presence of the malonic ester COOR"--CH 2 --COOR" and of an alcoholic solvent R"OH, the alkylating agent being in substantially equimolar ratio with respect to said epoxide and the malonic ester being in a molar ratio, with respect to said epoxide, of from 0.5 to 2, an alpha-carbalkoxy-gamma-alkyl-lactone being thus obtained having the formula: ##STR23## (b) said carbalkoxy-alkyl-lactone (IV) is saponified in an alkaline medium, thereby obtaining the corresponding acid, and such acid is decarboxylated, at 100°-160° C., thereby obtaining a gamma-alkyl-lactone having formula (V).
Claim 2
Dependent Claim 243 words
A process for the preparation of a 2-alkylcyclopenten-2-one having formula: where R is C n H 2n+1 (linear or branched); (CH 2 ) n --COOR'; (CH 2 ) n --NR' 2 ; (CH 2 ) n --OR'; (CH 2 ) n X or (CH 2 ) n --CN, n ranges from 1 to 20, X is Cl, Br, I or F, and R' is an alkyl group containing up to 5 carbon atoms, a benzyl group, or a phenyl group, the last two groups having optionally one or more substituent groups on the ring, wherein a saturated gamma-alkyl-lactone: ##STR21## is reacted at 20°-100° C. with a protic acid, thereby obtaining, by rearrangement, a 2-alkyl-cyclopenten-2-one (I), characterized in that said gamma-alkyl-lactone (V) is obtained through the following steps: (a) an epoxide: ##STR22## is made to react with an alkylating agent having the formula Na + [CH(COOR") 2 ] - (R" being an ethyl, isopropyl or isobutyl radical), in the presence of the malonic ester COOR"--CH 2 --COOR" and of an alcoholic solvent R"OH, the alkylating agent being in substantially equimolar ratio with respect to said epoxide and the malonic ester being in a molar ratio, with respect to said epoxide, of from 0.5 to 2, an alpha-carbalkoxy-gamma-alkyl-lactone being thus obtained having the formula: ##STR23## (b) said carbalkoxy-alkyl-lactone (IV) is saponified in an alkaline medium, thereby obtaining the corresponding acid, and such acid is decarboxylated, at 100°-160° C., thereby obtaining a gamma-alkyl-lactone having formula (V).
Claim 3
Dependent Claim 13 words
A process according to claim 1, wherein n ranges from 1 to 10.
Claim 4
Dependent Claim 27 words
A process according to claim 1 or 2, wherein R is selected from the class consisting of C n H 2n+1 and (CH 2 ) n --COOR'.
Claim 5
Dependent Claim 31 words
A process according to claim 1 or 2, wherein, in the second step (b), the malonic ester is used in a molar ratio, with respect to the epoxide, of about 1.
Claim 6
Dependent Claim 23 words
A process according to claim 1 or 2, wherein, in the fourth step (d), the acid is decarboxylated at 120° to 140° C.
Claim 7
Dependent Claim 21 words
A process according to claim 1 or 2, wherein the fifth step (e) is carried out at 50° to 60° C.
Claim 8
Dependent Claim 43 words
A process according to claim 1 or 2, wherein, in the fifth step (e), the protic acid is selected from the class consisting of a mixture of CH 3 --SO 3 H and P 2 O 5 , polyphosphoric acid, and sulphuric acid.
Claim 9
Dependent Claim 34 words
A process according to claim 7, wherein the protic acid is a mixture consisting of CH 3 -SO 3 H and P 2 O 5 , in a weight ratio from 10 to 20.
Claim 10
Dependent Claim 12 words
A process according to claim 8, wherein said ratio is about 10.

References Cited (Backward Citations)

US3299100A Cited
US3755370A Cited
US4229353A Cited
US4138584A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-06-15 1990-12-15 1991-06-16 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-06-15 1994-12-15 1995-06-16 $3760.00 Window Closed / Lapsed
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