CAS: 13553-79-2; 2,7-(Epoxypentadeca[1,11,13]Trienimino)Naphtho[2,1-B]Furan-1,6,9,11(2H)-Tetrone, 5,17,19,21-Tetrahydroxy-23-Methoxy-2,4,12,16,18,20,22-Heptamethyl-, 21-Acetate

上下游产品

R)-2-((S)-1-hydroxy-ethyl)-pyrrolidin-1-yl]-4-deoxy-rifamycin4-[(2R)-2-((S)-1-hydroxy-ethyl)-pyrrolidin-1-yl]-4-deoxy-rifamycin rifamycin B rifamycin O 3-(carbomethoxy)rifamycin S 3-(2-aminoethylthio)rifamycin SV rifamycin Verde

二恶酮利福霉素 以 Aq. Phosphate Buffer,二甲基亚砜 用作溶剂,化学反应 1.0H,反应生成利福霉素
参考文献:一锅法合成利福霉素s避免氯化溶剂的工艺研究
标题:一锅法合成利福霉素s避免氯化溶剂的工艺研究
摘要:通过利福霉素b的氧化,从利福霉素b(抗生素安沙霉素家族的一个成员)轻松合成利福霉素s.目前在工业规模上,使用苛刻的ph条件和氯化溶剂进行该氧化.随着合适的缓冲液/甲醇系统的发展,与目前的方法相比,可以放弃氯化溶剂,获得相似的收率和时空收率.在该方法中使用甲醇作为反应介质对于在温和的反应条件下获得高收率至关重要.通过这种方法,一步就可以达到189 G L-1 H-1的利福霉素s的时空产率.
Doi:10.1021/acs.Oprd.5B00070

专利信息

专利号:US-4557866-A
优先权日:1984-05-15
标 题 :Process for the synthesis of pyrido-imidazo rifamycins
发明人：CANNATA VINCENZO; TAMAGNONE GIAN F
权利人:ALFA FARMACEUTICI SPA
摘要:A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen, nitro, mercapto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1-4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups. The process comprises reacting the rifamycin O of formula II with a 2-aminopyridine of formula III wherein R1 and R2 have the same meanings as before.

专利号:US-4743619-A
优先权日:1985-08-29
标 题 :Method of treating hepatitis
发明人：HUNG PAUL P
权利人:AMERICAN HOME PROD
摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-deoxo-4-imino-rifamycin S, (b) 3-amino-4-deoxo-4-[(4-aminophenyl)sulfonyl]amino-rifamycin SV, (c) 4-O-(n-butylsulfonyl)-3-[(1-piperidinylimino)methyl]-rifamycin SV, (d) 4-O-(n-butylsulfonyl)-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV, and (f) 4-deoxo-N,3-ethylidenimino-4-(methylsulfonyl)amino-rifamycin SV, said amount being effective to alleviate the effects of said hepatitis B virus. Also disclosed is a method of inhibiting the viral polymerase of hepatitis B virus by subjecting said polymerase to an amount of one of the rifamycin derivatives (a)-(f) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase. Compounds (b)-(f) described above are novel compounds.

专利号:US-4631290-A
优先权日:1985-08-29
标 题 :Method of treating hepatitis
发明人：HUNG PAUL P
权利人:AMERICAN HOME PROD
摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-deoxo-4-imino-rifamycin S, (b) 3-amino-4-deoxo-4-[(4-aminophenyl)sulphonyl]amino-rifamycin SV, (c) 4-O-n-butylsulphonyl-3-[(1-piperidinylimino)methyl]-rifamycin SV, (d) 4-O-n-butylsulfonyl-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV said amount being effective to alleviate the effects of said hepatitis B virus. Also disclosed is a method of inhibiting the viral polymerase of hepatitis B virus by subjecting said polymerase to an amount of one of the rifamycin derivatives (a)-(e) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase.

专利号:US-9150590-B2
优先权日:2011-05-19
标 题 :Process for the synthesis of rifaximin and a new pseudo-crystalline form of rifaximin obtained thereby
发明人：MAZZOLA DISMA; MOIANA SILVIA; COPPI GERMANO
权利人:MAZZOLA DISMA; MOIANA SILVIA; COPPI GERMANO; FRIULCHEM SPA
摘要:Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo-crystalline form of rifaximin with fewer impurities obtained thereby.

专利号:US-2014155422-A1
优先权日:2011-05-19
标题:New Process for the Synthesis of Rifaximin and a New Pseudo-Crystalline Form of Rifaximin Obtained Thereby

专利号:PT-117254-B
优先权日:2021-05-26
标题 :METHOD FOR SYNTHESIS OF 9-AMINOMETHYL TETRACYCLINE COMPOUNDS