US4277401A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Total synthesis of 1RS,4SR,5RS-4-(4,8-dimethyl)-5-hydroxy-7-nonen-1-yl)-4-methyl-3,8-dioxabicyclo[3.2.1]octane-1-acetic acid
Assignee: Ortho Pharmaceutical Corp
•
Filing: 1980-08-25
•
Granted: 1981-07-07
•
Expires: 2000-08-25
Abstract
Abstract The synthesis of 1RS,4SR,5RS-4-(4,8-dimethyl-5-hydroxy-7-nonen-1-yl)-4-methyl-3,8-dioxabicyclo[3.2.1]octane-1-acetic acid is described. The bicyclo acetic acid compound is useful as a uteroevacuant agent.
Inventors
- 👤 Zoltan G. Hajos
- 👤 Seymour Levine
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 08:23
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/02; C07D307/26; C07D307/30; C07D307/32; C07D307/33; A; A61; A61P; A61P15/00; A61P15/04; C07C; C07C45/00; C07C45/56; C07C45/57; C07C45/58; C07D307/04; C07D307/18; C07D307/20; C07D407/00; C07D407/02; C07D407/04; C07D493/00; C07D493/02; C07D493/08
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
305 words
The process for the preparation of a compound of the formula ##STR3## which comprises reacting a compound of the formula ##STR4## first with potassium acetate and then with diazomethane to form a compound of the formula ##STR5## reacting the ketone with a compound of the formula (C.sub.6 H.sub.5).sub.3 P═CH.sub.2 to form a compound of the formula ##STR6## hydrolyzing the ester with a base to form a compound of the formula ##STR7## oxidizing the hydroxy acid with a first oxidizing agent and treating the resulting product with an alcohol in the presence of an acid to form a compound of the formula ##STR8## reacting the bis-hydroxymethyl compound with an alcohol in the presence of acid to form a compound of the formula ##STR9## reacting the hydroxy ester with a second oxidizing agent, reacting the product formed with ethylene glycol and hydrolyzing the ester with a base to form a compound of the formula ##STR10## reacting the acid with borane-THF and the product formed with methanesulfonyl chloride to form a compound of the formula ##STR11## reacting the mesylate with a compound of the formula ##STR12## and hydrolyzing the ester to form a compound of the formula ##STR13## reacting the acid with 3-methyl-2-butenyl lithium, reacting the ketone formed with a reducing agent, hydrolyzing the hydroxy acetal with aqueous hydrochloric acid and esterifying the hydroxy compound with an esterifying agent to form a compound of the formula ##STR14## reacting the aldehyde with a compound of the formula (C.sub.6 H.sub.5).sub.3 P═CH.sub.2 reacting the product formed first with borane-THF followed by treatment with an alkali metal hydroxide and hydrogen peroxide, oxidizing the product formed with a third oxidizing agent, hydrolyzing the ester with a base and treating the salt formed with a mineral acid, wherein R is a lower alkanoyl group having 2-6 carbon atoms, and Ms is a mesyl group.
Claim 2
Dependent Claim
305 words
The process for the preparation of a compound of the formula ##STR3## which comprises reacting a compound of the formula ##STR4## first with potassium acetate and then with diazomethane to form a compound of the formula ##STR5## reacting the ketone with a compound of the formula (C.sub.6 H.sub.5).sub.3 P═CH.sub.2 to form a compound of the formula ##STR6## hydrolyzing the ester with a base to form a compound of the formula ##STR7## oxidizing the hydroxy acid with a first oxidizing agent and treating the resulting product with an alcohol in the presence of an acid to form a compound of the formula ##STR8## reacting the bis-hydroxymethyl compound with an alcohol in the presence of acid to form a compound of the formula ##STR9## reacting the hydroxy ester with a second oxidizing agent, reacting the product formed with ethylene glycol and hydrolyzing the ester with a base to form a compound of the formula ##STR10## reacting the acid with borane-THF and the product formed with methanesulfonyl chloride to form a compound of the formula ##STR11## reacting the mesylate with a compound of the formula ##STR12## and hydrolyzing the ester to form a compound of the formula ##STR13## reacting the acid with 3-methyl-2-butenyl lithium, reacting the ketone formed with a reducing agent, hydrolyzing the hydroxy acetal with aqueous hydrochloric acid and esterifying the hydroxy compound with an esterifying agent to form a compound of the formula ##STR14## reacting the aldehyde with a compound of the formula (C.sub.6 H.sub.5).sub.3 P═CH.sub.2 reacting the product formed first with borane-THF followed by treatment with an alkali metal hydroxide and hydrogen peroxide, oxidizing the product formed with a third oxidizing agent, hydrolyzing the ester with a base and treating the salt formed with a mineral acid, wherein R is a lower alkanoyl group having 2-6 carbon atoms, and Ms is a mesyl group.
Claim 3
Dependent Claim
12 words
The process of claim 1 wherein the hydrolyzing base is sodium hydroxide.
Claim 4
Dependent Claim
24 words
The process of claim 1 wherein the first oxidizing agent is potassium permanganate, the alcohol is methanol and the acid is conc. sulfuric acid.
Claim 5
Dependent Claim
13 words
The process of claim 1 wherein the second oxidizing agent is Jones reagent.
Claim 6
Dependent Claim
12 words
The process of claim 1 wherein the reducing agent is sodium borohydride.
Claim 7
Dependent Claim
12 words
The process of claim 1 wherein the esterifying agent is acetic anhydride.
Claim 8
Dependent Claim
21 words
The process of claim 1 wherein the alkali metal hydroxide is sodium hydroxide and the third oxidizing agent is Jones reagent.
Claim 9
Dependent Claim
12 words
The process of claim 1 wherein the mineral acid is hydrochloric acid.
Claim 10
Dependent Claim
9 words
The process of claim 1 wherein R is acetyl.
References Cited (Backward Citations)
US4102895A
Cited
US4215048A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-07-06 | 1985-01-05 | 1985-07-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-07-06 | 1989-01-05 | 1989-07-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-07-06 | 1993-01-05 | 1993-07-07 | $7700.00 | Window Closed / Lapsed |