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 PDF

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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
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IT
Italy
Prior art keywords
methoxyestradiol
purification
Prior art date
Application number
IT102022000012425A
Other languages
English (en)
Inventor
Roberto Lenna
Claudio Delfrate
Davide Rigamonti
Michele Boghi
Original Assignee
Ind Chimica Srl
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
Application filed by Ind Chimica Srl filed Critical Ind Chimica Srl
Priority to IT102022000012425A priority Critical patent/IT202200012425A1/it
Priority to FR2305880A priority patent/FR3136464B1/fr
Priority to CN202380053466.5A priority patent/CN119894916A/zh
Priority to EP23738863.2A priority patent/EP4536675B1/en
Priority to PCT/IB2023/056042 priority patent/WO2023242712A1/en
Priority to CA3259059A priority patent/CA3259059A1/en
Publication of IT202200012425A1 publication Critical patent/IT202200012425A1/it

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074Esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
IT102022000012425A 2022-06-13 2022-06-13 Processo per la purificazione di 2-metossiestradiolo da 4-metossiestradiolo ed intermedio del processo IT202200012425A1 (it)

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)

* Cited by examiner, † Cited by third party
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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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