IT202200012425A1 - Processo per la purificazione di 2-metossiestradiolo da 4-metossiestradiolo ed intermedio del processo - Google Patents
Processo per la purificazione di 2-metossiestradiolo da 4-metossiestradiolo ed intermedio del processo Download PDFInfo
- Publication number
- IT202200012425A1 IT202200012425A1 IT102022000012425A IT202200012425A IT202200012425A1 IT 202200012425 A1 IT202200012425 A1 IT 202200012425A1 IT 102022000012425 A IT102022000012425 A IT 102022000012425A IT 202200012425 A IT202200012425 A IT 202200012425A IT 202200012425 A1 IT202200012425 A1 IT 202200012425A1
- Authority
- IT
- Italy
- Prior art keywords
- methoxyestradiol
- purification
- Prior art date
Links
- 238000000034 method Methods 0.000 title 2
- CQOQDQWUFQDJMK-SSTWWWIQSA-N 2-methoxy-17beta-estradiol Chemical compound C([C@@H]12)C[C@]3(C)[C@@H](O)CC[C@H]3[C@@H]1CCC1=C2C=C(OC)C(O)=C1 CQOQDQWUFQDJMK-SSTWWWIQSA-N 0.000 title 1
- BCWZIZLVBYHFES-PYEWSWHRSA-N 4-methoxy-17beta-estradiol Chemical compound C([C@@H]12)C[C@]3(C)[C@@H](O)CC[C@H]3[C@@H]1CCC1=C2C=CC(O)=C1OC BCWZIZLVBYHFES-PYEWSWHRSA-N 0.000 title 1
- 238000000746 purification Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
- C07J1/0074—Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT102022000012425A IT202200012425A1 (it) | 2022-06-13 | 2022-06-13 | Processo per la purificazione di 2-metossiestradiolo da 4-metossiestradiolo ed intermedio del processo |
| FR2305880A FR3136464B1 (fr) | 2022-06-13 | 2023-06-09 | Procédé de purification de 2-méthoxyestradiol de 4-méthoxyestradiol et intermédiaires du procédé |
| CN202380053466.5A CN119894916A (zh) | 2022-06-13 | 2023-06-12 | 从4-甲氧基雌二醇纯化2-甲氧基雌二醇的方法及其中间体 |
| EP23738863.2A EP4536675B1 (en) | 2022-06-13 | 2023-06-12 | Process for the purification of 2-methoxyestradiol from 4- methoxyestradiol and intermediates of the process |
| PCT/IB2023/056042 WO2023242712A1 (en) | 2022-06-13 | 2023-06-12 | Process for the purification of 2-methoxyestradiol from 4- methoxyestradiol and intermediates of the process |
| CA3259059A CA3259059A1 (en) | 2022-06-13 | 2023-06-12 | PROCESS FOR THE PURIFICATION OF 2-METHOXYESTRADIOL FROM 4-METHOXYESTRADIOL AND PROCESS INTERMEDIARIES |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT102022000012425A IT202200012425A1 (it) | 2022-06-13 | 2022-06-13 | Processo per la purificazione di 2-metossiestradiolo da 4-metossiestradiolo ed intermedio del processo |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IT202200012425A1 true IT202200012425A1 (it) | 2023-12-13 |
Family
ID=83081449
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IT102022000012425A IT202200012425A1 (it) | 2022-06-13 | 2022-06-13 | Processo per la purificazione di 2-metossiestradiolo da 4-metossiestradiolo ed intermedio del processo |
Country Status (1)
| Country | Link |
|---|---|
| IT (1) | IT202200012425A1 (it) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001014405A2 (en) | 1999-08-23 | 2001-03-01 | Entremed, Inc. | Methods of obtaining 2-methoxyestradiol of high purity |
| US7037907B1 (en) * | 1999-10-14 | 2006-05-02 | The University Of Melbourne | Estradiol conjugates and uses thereof |
-
2022
- 2022-06-13 IT IT102022000012425A patent/IT202200012425A1/it unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001014405A2 (en) | 1999-08-23 | 2001-03-01 | Entremed, Inc. | Methods of obtaining 2-methoxyestradiol of high purity |
| US7037907B1 (en) * | 1999-10-14 | 2006-05-02 | The University Of Melbourne | Estradiol conjugates and uses thereof |
Non-Patent Citations (10)
| Title |
|---|
| CAS, no. 26788-23-8 |
| CHEN S-H ET AL: "A new synthetic route to 2- and 4-methoxyestradiols by nucleophilic substitution", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 47, no. 1, 1 January 1986 (1986-01-01), pages 63 - 81, XP023583051, ISSN: 0039-128X, [retrieved on 19860101], DOI: 10.1016/0039-128X(86)90077-2 * |
| FISHMAN J: "Synthesis of 2-Methoxyestrogens", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, vol. 80, 1 January 1958 (1958-01-01), pages 1213 - 1216, XP002200986, ISSN: 0002-7863, DOI: 10.1021/JA01538A050 * |
| H.-H. LI ET AL.: "Estradiol 17β and its metabolites stimulated celi proliferation and antagonize ascorbic acid-compressed celi proliferation in human ovarian cancer cells", SCIENCES, vol. 21, 2014, pages 102 - 111 |
| KIURU P S ET AL: "Short synthesis of 2-methoxyestradiol and 2-hydroxyestradiol", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 68, no. 4, 1 April 2003 (2003-04-01), pages 373 - 375, XP004429316, ISSN: 0039-128X, DOI: 10.1016/S0039-128X(03)00035-7 * |
| P. S. KIURU ET AL.: "short synthesis of 2-methoxylestradiol and 2-hydroxyestradiol", STEROIDS, vol. 68, 2003, pages 373 - 375, XP004429316, DOI: 10.1016/S0039-128X(03)00035-7 |
| STEROIDS, 2003 |
| T. H. LIPPERT: "the impact of endogenous estradiol metabolites on carcinogenesis", STEROIDS, vol. 65, 2000, pages 357 - 69, XP004222661, DOI: 10.1016/S0039-128X(00)00101-X |
| V. A. FRANDSEN: "Demonstration of 2-methoxyestrone and of 2-methoxyestradiol in human pregnancy urine", ACTA ENDOCRINOLOGICA, vol. 31, 1959, pages 603 - 7 |
| Y. H. CHENG ET AL.: "4-methoxyestradiol-induced oxidative injuries in human lung epelithals", TOXICOLOGY AND APPLIED PHARMACOLOGY, vol. 220, 2007, pages 271 - 277, XP022055961, DOI: 10.1016/j.taap.2007.01.024 |
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