GB935384A - Tetracycline derivatives and preparation thereof - Google Patents

Tetracycline derivatives and preparation thereof

Info

Publication number
GB935384A
GB935384A GB1728/60A GB172860A GB935384A GB 935384 A GB935384 A GB 935384A GB 1728/60 A GB1728/60 A GB 1728/60A GB 172860 A GB172860 A GB 172860A GB 935384 A GB935384 A GB 935384A
Authority
GB
United Kingdom
Prior art keywords
tetracycline
deoxy
amino
fluoro
hydrogen
Prior art date
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.)
Expired
Application number
GB1728/60A
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.)
Pfizer Inc
Original Assignee
Pfizer Inc
Charles Pfizer and Co Inc
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 Pfizer Inc, Charles Pfizer and Co Inc filed Critical Pfizer Inc
Publication of GB935384A publication Critical patent/GB935384A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Relates to aryl azo tetracycline compounds of the formula <FORM:0935384/IV(a)/1> or <FORM:0935384/IV(a)/2> and the N4-benzyl betaines thereof, wherein A is hydrogen or methyl, B and Q are each hydrogen or hydroxyl but when Q is hydroxyl A is methyl, D is hydrogen or dimethylamino, X is halogen and Ar is the organic residue of an aromatic diazonium salt having 6 to 12 carbon atoms, and also relates to the corresponding 7- or 9-amino-tetracycline compounds which may be obtained by reduction of the corresponding aryl diazo compound or nitro compound. These amino compounds may be converted to a diazonium salt and the diazonium group replaced by a desired substituent such as a cyano, fluoro, chloro, bromo, iodo, amino, cyanato, thiocyanato, nitro, arsenoxy mercapto, azido or alkylmercapto group. The Specification describes the preparation of many tetracycline derivatives of which the following are typical:- 7-phenylazotetracycline, 7-amino-tetracycline, 7-amino-6-deoxy-tetracycline, 7-chloro-6-deoxy-6-demethyl-tetracycline, 7-iodo-6-deoxy-tetracycline, 9-fluoro-6-deoxy-tetracycline, 7-cyano-6-deoxy-4-desdimethylaminotetracyline and 9-amino-tetracycline-7-fluoro- 6-deoxy-5-hydroxytetracycline. The tetracycline derivatives may be used in pharmaceutical compositions. Specification 885,760 is referred to.
GB1728/60A 1959-03-30 1960-01-18 Tetracycline derivatives and preparation thereof Expired GB935384A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US80265559A 1959-03-30 1959-03-30
US84786759A 1959-10-22 1959-10-22

Publications (1)

Publication Number Publication Date
GB935384A true GB935384A (en) 1963-08-28

Family

ID=27122477

Family Applications (1)

Application Number Title Priority Date Filing Date
GB1728/60A Expired GB935384A (en) 1959-03-30 1960-01-18 Tetracycline derivatives and preparation thereof

Country Status (2)

Country Link
FR (1) FR487M (en)
GB (1) GB935384A (en)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010017470A1 (en) * 2008-08-08 2010-02-11 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
US8088755B2 (en) * 2005-02-04 2012-01-03 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
AU2013200565B2 (en) * 2008-08-08 2015-07-09 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
US9315451B2 (en) 2009-05-08 2016-04-19 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
WO2016065290A1 (en) * 2014-10-23 2016-04-28 Tetraphase Pharmaceuticals, Inc. Semi-synthesis procedures
US9573895B2 (en) 2012-08-31 2017-02-21 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US9624166B2 (en) 2009-08-28 2017-04-18 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US10961190B2 (en) 2016-10-19 2021-03-30 Tetraphase Pharmaceuticals, Inc. Crystalline forms of eravacycline
US11192866B2 (en) * 2004-05-21 2021-12-07 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof

Cited By (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11192866B2 (en) * 2004-05-21 2021-12-07 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
AU2006210406C1 (en) * 2005-02-04 2013-03-07 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
US8088755B2 (en) * 2005-02-04 2012-01-03 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
AU2006210406B2 (en) * 2005-02-04 2012-05-03 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
US8470804B2 (en) 2005-02-04 2013-06-25 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
AU2013200565B2 (en) * 2008-08-08 2015-07-09 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
EP3000805A1 (en) * 2008-08-08 2016-03-30 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
US8501716B2 (en) 2008-08-08 2013-08-06 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
CN102177134B (en) * 2008-08-08 2014-04-16 麻州四期制药公司 C7-fluoro substituted tetracycline compounds
EP2682387A3 (en) * 2008-08-08 2014-06-18 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
US8796245B2 (en) 2008-08-08 2014-08-05 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
TWI453183B (en) * 2008-08-08 2014-09-21 Tetraphase Pharmaceuticals Inc C7-fluoro substituted tetracycline compounds
US8906887B2 (en) 2008-08-08 2014-12-09 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
JP2015120723A (en) * 2008-08-08 2015-07-02 テトラフェース ファーマシューティカルズ，インコーポレイテッド C7-fluoro substituted tetracycline compounds
WO2010017470A1 (en) * 2008-08-08 2010-02-11 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
CN105367440A (en) * 2008-08-08 2016-03-02 四相制药公司 C7-fluoro substituted tetracycline compounds
JP2011530534A (en) * 2008-08-08 2011-12-22 テトラフェース ファーマシューティカルズ，インコーポレイテッド C7-fluoro substituted tetracycline compounds
AU2015203286B2 (en) * 2008-08-08 2016-12-15 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
AU2009279473B2 (en) * 2008-08-08 2012-12-13 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
US9315451B2 (en) 2009-05-08 2016-04-19 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US10072007B2 (en) 2009-05-08 2018-09-11 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US9624166B2 (en) 2009-08-28 2017-04-18 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US9573895B2 (en) 2012-08-31 2017-02-21 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
CN108276404A (en) * 2012-08-31 2018-07-13 四相制药公司 Tetracycline compounds
US10913712B2 (en) 2012-08-31 2021-02-09 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US10315992B2 (en) 2012-08-31 2019-06-11 Tetraphase Pharmaceuticals, Inc. Tetracyline compounds
WO2016065290A1 (en) * 2014-10-23 2016-04-28 Tetraphase Pharmaceuticals, Inc. Semi-synthesis procedures
US10618879B2 (en) 2014-10-23 2020-04-14 Tetraphase Pharmaceuticals, Inc. Semi-synthesis procedures
US10087157B2 (en) 2014-10-23 2018-10-02 Tetraphase Pharmaceuticals, Inc. Semi-synthesis procedures
US10961190B2 (en) 2016-10-19 2021-03-30 Tetraphase Pharmaceuticals, Inc. Crystalline forms of eravacycline
US11578044B2 (en) 2016-10-19 2023-02-14 Tetraphase Pharmaceuticals, Inc. Crystalline forms of eravacycline

Also Published As

Publication number Publication date
FR487M (en) 1961-05-08

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