ES2915058R1 - Proceso para preparar (15alfa,16alfa,17beta)-estra-1,3,5(10)-trieno-3,15,16,17-tetrol (Estetrol) e intermedios de dicho proceso - Google Patents

Proceso para preparar (15alfa,16alfa,17beta)-estra-1,3,5(10)-trieno-3,15,16,17-tetrol (Estetrol) e intermedios de dicho proceso

Info

Publication number: ES2915058R1
Authority: ES; Spain
Prior art keywords: 15alpha; estetrol; 16alpha; 17beta; estra
Prior art date: 2019-09-27
Legal status (The legal status 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 status listed.): Granted

Application number

ES202290021A

Other languages

English (en)

Other versions

ES2915058B2 (es

ES2915058A2 (es

Inventor

Roberto Lenna

Andrea Fasana

Riccardo Lucentini

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Industriale Chimica SRL

Original Assignee

Industriale 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.)

2019-09-27

Filing date

2020-09-25

Publication date

2023-12-11

2019-09-27 Priority claimed from IT102019000017414A external-priority patent/IT201900017414A1/it

2019-11-22 Priority claimed from IT102019000021879A external-priority patent/IT201900021879A1/it

2020-09-25 Application filed by Industriale Chimica SRL filed Critical Industriale Chimica SRL

2022-06-20 Publication of ES2915058A2 publication Critical patent/ES2915058A2/es

2023-12-11 Publication of ES2915058R1 publication Critical patent/ES2915058R1/es

2024-06-21 Application granted granted Critical

2024-06-21 Publication of ES2915058B2 publication Critical patent/ES2915058B2/es

Status Active legal-status Critical Current

2040-09-25 Anticipated expiration legal-status Critical

Links

AJIPIJNNOJSSQC-UHFFFAOYSA-N (15alpha,16alpha,17beta)-Estra-1,3,5(10)-triene-3,15,16,17-tetrol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4O)O)C4C3CCC2=C1 AJIPIJNNOJSSQC-UHFFFAOYSA-N 0.000 title 1
AJIPIJNNOJSSQC-NYLIRDPKSA-N estetrol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)[C@@H]4O)O)[C@@H]4[C@@H]3CCC2=C1 AJIPIJNNOJSSQC-NYLIRDPKSA-N 0.000 title 1
229950009589 estetrol Drugs 0.000 title 1
239000000543 intermediate Substances 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
- 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
- C07J1/0003—Androstane derivatives
- C07J1/0007—Androstane derivatives not substituted in position 17
- 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
- C07J75/00—Processes for the preparation of steroids in general

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Steroid Compounds (AREA)
Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

ES202290021A 2019-09-27 2020-09-25 Proceso para preparar (15alfa,16alfa,17beta)-estra-1,3,5(10)-trieno-3,15,16,17-tetrol (Estetrol) e intermedios de dicho proceso Active ES2915058B2 (es)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
IT102019000017414A IT201900017414A1 (it)	2019-09-27	2019-09-27	Processo per la preparazione di (15α,16α,17β)-estra-1,3,5(10)-triene-3,15,16,17-tetrolo (Estetrolo) ed intermedi di detto processo
IT102019000021879A IT201900021879A1 (it)	2019-11-22	2019-11-22	PROCESSO PER LA PREPARAZIONE DI (15α,16α,17β)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROLO (ESTETROLO) ED INTERMEDI DI DETTO PROCESSO
PCT/EP2020/076843 WO2021058716A1 (en)	2019-09-27	2020-09-25	Process for preparing (15αlpha,16αlpha,17βeta)-estra-1,3,5(10)-triene-3,15,16,17-tetrol (estetrol) and intermediates of said process

Publications (3)

Publication Number	Publication Date
ES2915058A2 ES2915058A2 (es)	2022-06-20
ES2915058R1 true ES2915058R1 (es)	2023-12-11
ES2915058B2 ES2915058B2 (es)	2024-06-21

Family

ID=72895895

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ES202290021A Active ES2915058B2 (es)	2019-09-27	2020-09-25	Proceso para preparar (15alfa,16alfa,17beta)-estra-1,3,5(10)-trieno-3,15,16,17-tetrol (Estetrol) e intermedios de dicho proceso

Country Status (15)

Country	Link
US (1)	US20220348607A1 (es)
JP (1)	JP2022549585A (es)
CN (1)	CN116355031A (es)
AU (2)	AU2020355615B2 (es)
BR (1)	BR112022005359A2 (es)
CA (1)	CA3151465C (es)
CH (1)	CH718008B1 (es)
DE (1)	DE112020004564T5 (es)
ES (1)	ES2915058B2 (es)
FR (2)	FR3101348B1 (es)
GB (2)	GB2617040B (es)
MX (2)	MX2022003688A (es)
UY (1)	UY38895A (es)
WO (1)	WO2021058716A1 (es)
ZA (1)	ZA202204137B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
HU231240B1 (hu) *	2019-09-03	2022-04-28	Richter Gedeon Nyrt.	Ipari eljárás nagytisztaságú ösztetrol hatóanyag előállítására
GB2626482A (en) *	2021-10-01	2024-07-24	Ind Chimica Srl	Process for preparing (15alpha,16alpha,17eta)-estra-1,3,5-(10)-triene-3,15,16,17-tetrol(estetrol) monohydrate

Citations (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2004041839A2 (en) *	2002-11-08	2004-05-21	Pantarhei Bioscience B.V.	Synthesis of estetrol via estrone derived steroids
WO2015040051A1 (en) *	2013-09-18	2015-03-26	Crystal Pharma, S.A.U.	Process for the preparation of estetrol
ES2855923T3 (es) *	2019-09-03	2023-04-28	Richter Gedeon Nyrt	Procedimiento industrial para la preparación de estetrol de alta pureza

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
HUE029252T2 (en)	2011-06-01	2017-02-28	Estetra Sprl	Process for the preparation of intermediates of estetrol
EP2383279A1 (en) *	2011-07-19	2011-11-02	Pantarhei Bioscience B.V.	Process for the preparation of estetrol
MX348917B (es)	2011-10-07	2017-07-04	Estetra Sprl	Proceso para la producción de estetrol.

2020
- 2020-09-25 MX MX2022003688A patent/MX2022003688A/es unknown
- 2020-09-25 JP JP2022515787A patent/JP2022549585A/ja active Pending
- 2020-09-25 GB GB2310271.8A patent/GB2617040B/en active Active
- 2020-09-25 GB GB2205967.9A patent/GB2603868B/en active Active
- 2020-09-25 CN CN202310346726.XA patent/CN116355031A/zh active Pending
- 2020-09-25 AU AU2020355615A patent/AU2020355615B2/en active Active
- 2020-09-25 BR BR112022005359A patent/BR112022005359A2/pt unknown
- 2020-09-25 US US17/763,267 patent/US20220348607A1/en active Pending
- 2020-09-25 DE DE112020004564.1T patent/DE112020004564T5/de active Pending
- 2020-09-25 WO PCT/EP2020/076843 patent/WO2021058716A1/en active Application Filing
- 2020-09-25 UY UY0001038895A patent/UY38895A/es unknown
- 2020-09-25 CA CA3151465A patent/CA3151465C/en active Active
- 2020-09-25 FR FR2009758A patent/FR3101348B1/fr active Active
- 2020-09-25 CH CH000332/2022A patent/CH718008B1/it unknown
- 2020-09-25 ES ES202290021A patent/ES2915058B2/es active Active
2022
- 2022-03-25 MX MX2023004110A patent/MX2023004110A/es unknown
- 2022-04-12 ZA ZA2022/04137A patent/ZA202204137B/en unknown
2023
- 2023-02-24 FR FR2301733A patent/FR3132908A1/fr active Pending
- 2023-04-12 AU AU2023202251A patent/AU2023202251A1/en active Pending

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2004041839A2 (en) *	2002-11-08	2004-05-21	Pantarhei Bioscience B.V.	Synthesis of estetrol via estrone derived steroids
WO2015040051A1 (en) *	2013-09-18	2015-03-26	Crystal Pharma, S.A.U.	Process for the preparation of estetrol
ES2855923T3 (es) *	2019-09-03	2023-04-28	Richter Gedeon Nyrt	Procedimiento industrial para la preparación de estetrol de alta pureza

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
FISHMAN, J. & GUZIK, H. . ¿Synthesis of Epimeric 15-Hydroxyestriols, New and Potential Metabolites of Estradiol¿. Journal of Organic Chemistry, 1968, Vol. 33, Páginas 3133-3135 0022-3263; 1520-6904 (en línea) , (DOI: 10.1021/jo01272a023) Ver página 3133, figura; página 3135, columna 1, párrafo 3-columna 2, párrafo 1. *

Also Published As

Publication number	Publication date
JP2022549585A (ja)	2022-11-28
GB2603868A (en)	2022-08-17
US20220348607A1 (en)	2022-11-03
GB2617040A (en)	2023-09-27
DE112020004564T5 (de)	2022-06-15
GB202310271D0 (en)	2023-08-16
CA3151465C (en)	2024-05-07
BR112022005359A2 (pt)	2022-07-19
FR3101348B1 (fr)	2024-01-19
WO2021058716A1 (en)	2021-04-01
ZA202204137B (en)	2023-06-28
CA3151465A1 (en)	2021-04-01
AU2020355615B2 (en)	2023-12-14
FR3132908A1 (fr)	2023-08-25
ES2915058B2 (es)	2024-06-21
GB202205967D0 (en)	2022-06-08
UY38895A (es)	2021-04-30
AU2023202251A1 (en)	2023-05-04
CH718008B1 (it)	2024-01-31
FR3101348A1 (fr)	2021-04-02
AU2020355615A1 (en)	2022-05-19
ES2915058A2 (es)	2022-06-20
GB2603868B (en)	2023-10-11
CN114514237A (zh)	2022-05-17
CN116355031A (zh)	2023-06-30
GB2617040B (en)	2024-03-27
MX2023004110A (es)	2023-04-27
MX2022003688A (es)	2022-04-26

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