HRP20160692T2 - Postupak za proizvodnju intermedijera estetrola - Google Patents
Postupak za proizvodnju intermedijera estetrola Download PDFInfo
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- HRP20160692T2 HRP20160692T2 HRP20160692TT HRP20160692T HRP20160692T2 HR P20160692 T2 HRP20160692 T2 HR P20160692T2 HR P20160692T T HRP20160692T T HR P20160692TT HR P20160692 T HRP20160692 T HR P20160692T HR P20160692 T2 HRP20160692 T2 HR P20160692T2
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- 238000000034 method Methods 0.000 title claims 18
- 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 claims 3
- 229950009589 estetrol Drugs 0.000 title claims 3
- 239000000543 intermediate Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- -1 C1−6alkylene carbonate Chemical compound 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- PIBWKRNGBLPSSY-UHFFFAOYSA-L palladium(II) chloride Chemical compound Cl[Pd]Cl PIBWKRNGBLPSSY-UHFFFAOYSA-L 0.000 claims 3
- YJVFFLUZDVXJQI-UHFFFAOYSA-L palladium(ii) acetate Chemical compound [Pd+2].CC([O-])=O.CC([O-])=O YJVFFLUZDVXJQI-UHFFFAOYSA-L 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 239000003638 chemical reducing agent Substances 0.000 claims 2
- 229910052987 metal hydride Inorganic materials 0.000 claims 2
- 239000012279 sodium borohydride Substances 0.000 claims 2
- 229910000033 sodium borohydride Inorganic materials 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 229910004664 Cerium(III) chloride Inorganic materials 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 229910010084 LiAlH4 Inorganic materials 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- VYLVYHXQOHJDJL-UHFFFAOYSA-K cerium trichloride Chemical compound Cl[Ce](Cl)Cl VYLVYHXQOHJDJL-UHFFFAOYSA-K 0.000 claims 1
- NBWIIOQJUKRLKW-UHFFFAOYSA-N chloro(phenyl)silane Chemical compound Cl[SiH2]C1=CC=CC=C1 NBWIIOQJUKRLKW-UHFFFAOYSA-N 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 239000012280 lithium aluminium hydride Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- PZABZCASVQXUET-UHFFFAOYSA-N phenylsilyl trifluoromethanesulfonate Chemical compound FC(F)(F)S(=O)(=O)O[SiH2]C1=CC=CC=C1 PZABZCASVQXUET-UHFFFAOYSA-N 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J75/00—Processes for the preparation of steroids in general
-
- 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
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- 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
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (14)
1. Postupak za pripravu spoja formule (I)
[image]
pri čemu navedeni postupak sadrži sljedeće korake:
a) reakciju spoja formule (II) sa acilirajućim ili sililirajućim sredstvom kako bi se dobio spoj formule (III), gdje su P¹ i P² svaki nezavisna zaštitna skupina odabrana iz R²-Si-R³R⁴, ili R¹CO-, pri čemu je R¹ skupina odabrana iz C₁₋₆alkila ili C₃₋₆cikloalkila, a svaka skupina po izboru je supstituirana sa jednim ili više supstituenata nezavisno odabranih između fluoro ili C₁₋₄alkila; svaki od R², R³ i R⁴ su nezavisna skupina odabrana između C₁₋₆alkila ili fenila, a svaka skupina po izboru je supstituirana sa jednim ili više supstituenata nezavisno odabranih između fluoro ili C₁₋₄alkila;
[image]
b) reakciju spoja formule (III), u prisustvu paladij acetata ili paladij klorida kako bi se dobio spoj formule (IV); i
[image]
c) reakciju spoja formule (IV) s redukcijskim sredstvom kako bi se dobio spoj formule (I).
2. Postupak prema zahtjevu 1, pri čemu P¹ predstavlja R¹CO-.
3. Postupak prema zahtjevu 1, pri čemu P¹ predstavlja R²-Si-R³R⁴.
4. Postupak prema zahtjevu 3, pri čemu P² predstavlja R²-Si-R³R⁴.
5. Postupak prema bilo kojem od zahtjeva 1 do 3, pri čemu P² predstavlja R¹CO-.
6. Postupak prema zahtjevu 5, u kome korak (a) obuhvaća sljedeće korake: (a1) zaštitu hidroksilne skupine spoja formule (II) sa sililirajućim sredstvom čime se dobije spoj formule (IIa), pri čemu P1 ima istu vrijednost kao što je definirano u zahtjevu 3; i
[image]
(a2) zaštitu ketona spoja formule (IIa), u prisustvu acilirajućeg sredstva kako bi se dobio spoj formule (III).
7. Postupak prema bilo kojem od zahtjeva 1 do 3, 5, i 6, u kome je acilirajuće sredstvo C₂₋₆alkenilC₁₋₆alkanoat ili
C₂₋₆alkenilC₃₋₆cikloalkanoat.
8. Postupak prema bilo kojem od zahtjeva 1, 3 do 7, u kome se sredstvo za sililiranje odabire iz skupine koju čine C₁₋₆alkilsililklorid, C₁₋₆alkilsililtriflat, fenilsilil klorid, fenilsililtriflat, C₁₋₆alkilfenilsililklorid, C₁₋₆alkilfenilsililtriflat, svaka skupina po izboru je supstituirana sa jednim ili više supstituenata nezavisno odabranih između fluoro ili C₁₋₄alkila.
9. Postupak prema bilo kojem od zahtjeva 1 do 8, u kome se korak (b) provodi u prisutnosti C₁₋₆alkilen karbonata formule Rb-O-CO-O-Ra gdje je Ra C₁₋₆-alkil, a Rb je C₂₋₆ alkenil, i organokositreni spoj.
10. Postupak prema bilo kojem od zahtjeva 1 do 9, u kome je paladij acetat ili paladij klorid prisutan u stehiometrijskim količinama.
11. Postupak prema bilo kojem od zahtjeva 1 do 9, u kome se spomenuta reakcija izvodi sa paladij acetatom i paladij kloridom prisutnom u katalitičkim ili sub-stehiometrijskim količinama, poželjno je da se reakcija izvodi u atmosferi kisika.
12. Postupak prema bilo kojem od zahtjeva 1 do 11, u kome se redukcijsko sredstvo u koraku (c) odabire iz skupine koju čine spojevi metalnih hidrida.
13. Postupak prema zahtjevu 12, u kome je spoj metalnog hidrida odabran iz skupine koju čine NaBH₄/CeCl₃, LiAlH₄, NaBH₄, NaBH(OAc )₃ i ZnBH₄.
14. Postupak za pripravu estetrola, koji postupak obuhvaća pripravu spoja formule (I) postupkom prema bilo kojem od zahtjeva 1 do 13, a dalje obuhvaća reakciju spoja formule (I) kako bi se proizveo estetrol.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161492300P | 2011-06-01 | 2011-06-01 | |
EP11168561 | 2011-06-01 | ||
EP12729054.2A EP2714710B1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
PCT/EP2012/060447 WO2012164096A1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP20160692T1 HRP20160692T1 (hr) | 2016-08-12 |
HRP20160692T2 true HRP20160692T2 (hr) | 2016-09-23 |
Family
ID=45003353
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20160692TT HRP20160692T2 (hr) | 2011-06-01 | 2016-06-17 | Postupak za proizvodnju intermedijera estetrola |
Country Status (24)
Country | Link |
---|---|
US (1) | US11053274B2 (hr) |
EP (1) | EP2714710B1 (hr) |
JP (2) | JP6425540B2 (hr) |
KR (1) | KR101994805B1 (hr) |
CN (2) | CN107266514A (hr) |
AU (1) | AU2012264602B2 (hr) |
BR (1) | BR112013030830B1 (hr) |
CA (1) | CA2835981C (hr) |
CY (1) | CY1118150T1 (hr) |
DK (1) | DK2714710T3 (hr) |
EA (1) | EA023991B1 (hr) |
ES (1) | ES2579175T3 (hr) |
HR (1) | HRP20160692T2 (hr) |
HU (1) | HUE029252T2 (hr) |
ME (1) | ME02454B (hr) |
MX (1) | MX341561B (hr) |
PL (1) | PL2714710T3 (hr) |
PT (1) | PT2714710T (hr) |
RS (1) | RS54880B1 (hr) |
SG (1) | SG195118A1 (hr) |
SI (1) | SI2714710T1 (hr) |
SM (1) | SMT201600206B (hr) |
WO (1) | WO2012164096A1 (hr) |
ZA (1) | ZA201308446B (hr) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RS55293B1 (sr) | 2011-06-01 | 2017-03-31 | Estetra Sprl | Postupak proizvodnje intermedijara estetrola |
JP6425540B2 (ja) | 2011-06-01 | 2018-11-21 | エステトラ エス.ペ.エール.エル. | エステトロール中間体を製造するための方法 |
EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
ES2593316T3 (es) | 2011-10-07 | 2016-12-07 | Estetra S.P.R.L. | Proceso para la producción de Estetrol |
CN107750157B (zh) | 2015-06-18 | 2021-07-13 | 埃斯特拉私人有限责任公司 | 含雌四醇的口腔分散片剂 |
ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
LT3106148T (lt) | 2015-06-18 | 2018-06-25 | Mithra Pharmaceuticals S.A. | Burnoje disperguojamos dozės vienetas, turintis estetrolio komponentą |
TN2017000497A1 (en) | 2015-06-18 | 2019-04-12 | Mithra Pharmaceuticals S A | Orodispersible dosage unit containing an estetrol component |
CN105837424A (zh) * | 2016-03-31 | 2016-08-10 | 常州大学 | 一种1-氯-3-甲基-3-丁烯-2-酮的合成方法 |
KR20220144885A (ko) | 2016-08-05 | 2022-10-27 | 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 | 월경통 및 생리통의 관리방법 |
JP6935766B2 (ja) | 2018-02-15 | 2021-09-15 | 日本精工株式会社 | スピンドル装置 |
JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
IT201900021879A1 (it) | 2019-11-22 | 2021-05-22 | Ind Chimica Srl | 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 |
IT201900017414A1 (it) | 2019-09-27 | 2021-03-27 | Ind Chimica Srl | 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 |
MX2022003688A (es) | 2019-09-27 | 2022-04-26 | Ind Chimica Srl | Proceso para preparar (15alfa,16alfa,17beta)-estra-1,3,5(10)-trien o-3,15,16,17-tetrol (estetrol) e intermedios de dicho proceso. |
WO2023021026A1 (en) | 2021-08-17 | 2023-02-23 | Aspen Oss B.V. | A synthetic pathway to estra-1,3,5(10)-triene-3,15a,16a,17b-tetrol |
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