AR090618A1 - Proceso para la preparacion de inhibidores de sglt2 de derivados de bencilbenceno - Google Patents
Proceso para la preparacion de inhibidores de sglt2 de derivados de bencilbencenoInfo
- Publication number
- AR090618A1 AR090618A1 ARP130101120A ARP130101120A AR090618A1 AR 090618 A1 AR090618 A1 AR 090618A1 AR P130101120 A ARP130101120 A AR P130101120A AR P130101120 A ARP130101120 A AR P130101120A AR 090618 A1 AR090618 A1 AR 090618A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkoxy
- alkyl
- cycloalkyl
- group
- alkynyloxy
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 title 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 19
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 13
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 7
- 150000001875 compounds Chemical class 0.000 abstract 7
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 6
- -1 alkyl magnesium Chemical compound 0.000 abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 239000011777 magnesium Substances 0.000 abstract 4
- 229910052749 magnesium Inorganic materials 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 3
- 239000011541 reaction mixture Substances 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 239000003960 organic solvent Substances 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001347 alkyl bromides Chemical class 0.000 abstract 1
- 150000001348 alkyl chlorides Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000001246 bromo group Chemical group Br* 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 229910052805 deuterium Inorganic materials 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 201000001421 hyperglycemia Diseases 0.000 abstract 1
- 229910052740 iodine Chemical group 0.000 abstract 1
- 239000011630 iodine Chemical group 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/02—Acyclic radicals, not substituted by cyclic structures
- C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C29/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
- C07C29/132—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group
- C07C29/136—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group of >C=O containing groups, e.g. —COOH
- C07C29/147—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group of >C=O containing groups, e.g. —COOH of carboxylic acids or derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C37/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
- C07C37/01—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by replacing functional groups bound to a six-membered aromatic ring by hydroxy groups, e.g. by hydrolysis
- C07C37/055—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by replacing functional groups bound to a six-membered aromatic ring by hydroxy groups, e.g. by hydrolysis the substituted group being bound to oxygen, e.g. ether group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C37/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
- C07C37/11—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by reactions increasing the number of carbon atoms
- C07C37/16—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by reactions increasing the number of carbon atoms by condensation involving hydroxy groups of phenols or alcohols or the ether or mineral ester group derived therefrom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
- C07C41/01—Preparation of ethers
- C07C41/18—Preparation of ethers by reactions not forming ether-oxygen bonds
- C07C41/30—Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/10—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
- C07C39/12—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings
- C07C39/15—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings with all hydroxy groups on non-condensed rings, e.g. phenylphenol
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
- C07C41/01—Preparation of ethers
- C07C41/16—Preparation of ethers by reaction of esters of mineral or organic acids with hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/225—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
- C07H7/04—Carbocyclic radicals
-
- 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)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- Emergency Medicine (AREA)
- Public Health (AREA)
- Obesity (AREA)
- Crystallography & Structural Chemistry (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyrane Compounds (AREA)
- Saccharide Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2012/073697 WO2013152476A1 (en) | 2012-04-10 | 2012-04-10 | Process for the preparation of benzylbenzene sglt2 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR090618A1 true AR090618A1 (es) | 2014-11-26 |
Family
ID=49326992
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130101120A AR090618A1 (es) | 2012-04-10 | 2013-04-05 | Proceso para la preparacion de inhibidores de sglt2 de derivados de bencilbenceno |
Country Status (16)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104478671B (zh) * | 2015-01-15 | 2016-03-09 | 佛山市赛维斯医药科技有限公司 | 一类双烷氧苯基丙二醇衍生物和用途 |
| CN104478675B (zh) * | 2015-01-15 | 2016-01-06 | 佛山市赛维斯医药科技有限公司 | 一类含烷氧苯基和三氟甲苯基丙二醇结构的衍生物和用途 |
| CN104478674B (zh) * | 2015-01-15 | 2016-03-09 | 佛山市赛维斯医药科技有限公司 | 一类烷氧苯基丙二醇衍生物和用途 |
| EP3256482B1 (en) | 2015-02-09 | 2019-11-27 | Indoco Remedies Limited | Process for the preparation of sglt inhibitor compounds |
| CZ2015729A3 (cs) * | 2015-10-13 | 2017-04-26 | Zentiva, K.S. | Příprava intermediátů pro syntézu Canagliflozinu a Dapagliflozinu |
| CN107641139A (zh) * | 2016-07-22 | 2018-01-30 | 江苏豪森药业集团有限公司 | 达格列净中间体的晶型及其制备方法 |
| WO2018207113A1 (en) * | 2017-05-09 | 2018-11-15 | Piramal Enterprises Limited | A process for the preparation of sglt2 inhibitor and intermediates thereof |
| US20190343853A1 (en) * | 2018-04-25 | 2019-11-14 | Theracos Sub, Llc | Methods of treating hypertension |
| CN114570303A (zh) * | 2022-03-02 | 2022-06-03 | 南京市计量监督检测院 | 微通道反应器及基于反应器制备达格列净中间体的方法 |
| WO2025056984A1 (en) * | 2023-09-12 | 2025-03-20 | Vijayasri Organics Private Limited | A novel process for the preparation of bexagliflozin a sglt2 inhibitor and its intermediates thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI254635B (en) * | 2002-08-05 | 2006-05-11 | Yamanouchi Pharma Co Ltd | Azulene derivative and salt thereof |
| BR0317929A (pt) * | 2003-01-03 | 2006-04-11 | Bristol Myers Squibb Co | métodos de produzir inibidores de sglt2 de glicosìdeo de c-arila |
| MXPA05009356A (es) * | 2003-03-14 | 2005-12-05 | Astellas Pharma Inc | Derivados de c-glicosido y sales de los mismos. |
| AR051446A1 (es) * | 2004-09-23 | 2007-01-17 | Bristol Myers Squibb Co | Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2) |
| TW200637839A (en) * | 2005-01-07 | 2006-11-01 | Taisho Pharmaceutical Co Ltd | 1-thio-d-glucitol derivatives |
| TW200845956A (en) * | 2006-12-18 | 2008-12-01 | Smithkline Beecham Corp | Calcilytic compounds |
| JP2010519273A (ja) * | 2007-02-21 | 2010-06-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 四置換グルコピラノシル化ベンゼン誘導体、このような化合物を含む薬物、それらの使用及びそれらの製造方法 |
| AU2008288770B2 (en) * | 2007-08-23 | 2014-06-12 | Theracosbio, Llc | Benzylbenzene derivatives and methods of use |
| SG193168A1 (en) * | 2008-08-22 | 2013-09-30 | Theracos Inc | Processes for the preparation of sglt2 inhibitors |
| US9056850B2 (en) * | 2008-10-17 | 2015-06-16 | Janssen Pharmaceutica N.V. | Process for the preparation of compounds useful as inhibitors of SGLT |
| CA2775961C (en) * | 2009-09-30 | 2017-11-07 | Boehringer Ingelheim International Gmbh | Method for the preparation of a crystalline form of 1-chloro-4-(beta-d-glucopyranos-1-yl)-2-(4-((s)-tetrahydrofuran-3-yloxy)benzyl)benzene |
| HRP20150945T1 (hr) * | 2009-09-30 | 2015-10-09 | Boehringer Ingelheim International Gmbh | Postupci za proizvodnju derivata benzil-benzena supstituiranog glukopiranozilom |
-
2012
- 2012-04-10 WO PCT/CN2012/073697 patent/WO2013152476A1/en active Application Filing
-
2013
- 2013-03-14 WO PCT/CN2013/072642 patent/WO2013152654A1/en active Application Filing
- 2013-03-14 CA CA2867057A patent/CA2867057C/en active Active
- 2013-03-14 RU RU2014144944A patent/RU2625795C2/ru active
- 2013-03-14 SG SG11201406434PA patent/SG11201406434PA/en unknown
- 2013-03-14 BR BR112014025105-3A patent/BR112014025105B1/pt active IP Right Grant
- 2013-03-14 EP EP13775129.3A patent/EP2836500A4/en not_active Withdrawn
- 2013-03-14 NZ NZ630408A patent/NZ630408A/en unknown
- 2013-03-14 AU AU2013247304A patent/AU2013247304B2/en active Active
- 2013-03-14 HK HK15107805.3A patent/HK1207084A1/xx unknown
- 2013-03-14 JP JP2015504847A patent/JP6208745B2/ja active Active
- 2013-03-14 MX MX2014012268A patent/MX353307B/es active IP Right Grant
- 2013-03-14 KR KR1020147031540A patent/KR102106310B1/ko not_active Expired - Fee Related
- 2013-04-05 AR ARP130101120A patent/AR090618A1/es unknown
- 2013-04-10 TW TW102112741A patent/TWI597289B/zh active
-
2014
- 2014-09-16 ZA ZA2014/06899A patent/ZA201406899B/en unknown
- 2014-09-22 IL IL234800A patent/IL234800B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| JP2015514118A (ja) | 2015-05-18 |
| KR102106310B1 (ko) | 2020-05-04 |
| EP2836500A1 (en) | 2015-02-18 |
| TW201402593A (zh) | 2014-01-16 |
| SG11201406434PA (en) | 2014-11-27 |
| RU2625795C2 (ru) | 2017-07-19 |
| TWI597289B (zh) | 2017-09-01 |
| CA2867057A1 (en) | 2013-10-17 |
| BR112014025105B1 (pt) | 2022-03-29 |
| KR20150001811A (ko) | 2015-01-06 |
| CA2867057C (en) | 2020-03-31 |
| NZ630408A (en) | 2016-09-30 |
| AU2013247304B2 (en) | 2017-03-30 |
| WO2013152654A1 (en) | 2013-10-17 |
| MX2014012268A (es) | 2015-03-09 |
| HK1207084A1 (en) | 2016-01-22 |
| EP2836500A4 (en) | 2016-03-23 |
| AU2013247304A1 (en) | 2014-09-25 |
| WO2013152476A1 (en) | 2013-10-17 |
| BR112014025105A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2017-06-20 |
| JP6208745B2 (ja) | 2017-10-04 |
| MX353307B (es) | 2018-01-08 |
| ZA201406899B (en) | 2023-07-26 |
| RU2014144944A (ru) | 2016-06-10 |
| IL234800B (en) | 2018-06-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |