Vardenafil Intermediate CAS 224789-21-3 Ubunyulu > 99.0% (HPLC)
I-Shanghai Ruifu Chemical Co., Ltd. ngumenzi okhokelayo we-2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-enye (I-CAS: 224789-21-3) enomgangatho ophezulu, ophakathi kweVardenafil.I-Ruifu Chemical inokubonelela ngenkonzo yehlabathi jikelele, ixabiso elikhuphisanayo, inkonzo egqwesileyo, encinci kunye nezixa ezininzi ezikhoyo.Thenga i-Vardenafil Intermediates,Please contact: alvin@ruifuchem.com
Igama leMchiza | 2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-enye |
Izithethantonye | Ukungcola kweVardenafil Dessulfonyl;I-2-(2-Ethoxyphenyl)-5-Methyl-7-Propyl-3H-Imidazo[5,1-F][1,2,4]triazin-4-enye;I-Vardenafil Propyl Imidazotriazinone Ukungcola;Vardenafil Related Compound 1 |
Ubume beStokhwe | KwiSitokhwe, Umthamo weMveliso iiToni ezi-2 ngenyanga |
Inombolo yeCAS | 224789-21-3 |
Ifomula yeemolekyuli | I-C17H20N4O2 |
Ubunzima beMolekyuli | 312.37 g/mol |
Indawo yokunyibilika | 142.0 ~ 148.0℃ |
Ukuxinana | 1.26±0.10 g/cm3 |
Ugcino Lwexesha elide | Indawo epholileyo neyomileyo (2~8℃) |
I-COA kunye ne-MSDS | Iyafumaneka |
Imvelaphi | Shanghai, China |
Uphawu | Ruifu Chemical |
Izinto | Iinkcukacha | Iziphumo |
Imbonakalo | Okumhlophe-kuMhlophe ukuya kwiPoda eLuthulu | I-Off-White Powder |
Indawo yokunyibilika | 142.0 ~ 148.0℃ | 146.0 ~ 147.0℃ |
Ilahleko ekomisweni | <1.00% (102℃, 3h) | 0.23% |
Iintsimbi ezinzima (Pb) | ≤20ppm | <20ppm |
Ubunyulu / Indlela yokuHlalutya | >99.0% (HPLC) | 99.79% |
I-1H NMR Spectrum | Ngokungqinelana noLwakhiwo | Iyahambelana |
Ukuqukumbela | Imveliso ivavanyiwe kwaye ihambelana neenkcukacha ezinikiweyo | |
Isicelo | Phakathi kweVardenafil / Vardenafil Hydrochloride |
Umqulu:Ibhotile, ingxowa yefoyile yeAluminiyam, 25kg/Igubu lekhadibhodi, okanye ngokwemfuno yomthengi.
Imeko yoGcino:Gcina isikhongozeli sivalwe ngokuqinileyo kwaye usigcine kwindawo epholileyo, eyomileyo (2~8℃) kunye nendawo yokugcina impahla engena moya ikude kwizinto ezingahambelaniyo.Khusela ekukhanyeni kwelanga kunye nokufuma.
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1. Imbonakalo: Beka isampulu kwiphepha elimhlophe kwaye ujonge inkangeleko, off-mhlophe ukuya kumgubo omthubi.
2. Uhlalutyo:
2.1 Ukumiselwa kwendawo enyibilikayo ngokomthetho (i-Chinese Pharmacopoeia 2010 Edition II Isihlomelo ⅥC) Indawo yokunyibilika yi-142.0~148.0℃.
2.2 Ilahleko ekomisweni: Ukumiselwa ngokomthetho (Isihlomelo ⅧL, iCandelo II, uHlelo luka-2010 lwe-Chinese Pharmacopoeia).Ukuchaneka kobunzima bexabiso elifanelekileyo le mveliso, yome kwi-102 ℃ kwiiyure ze-3, ukulahleka kwesisindo akuyi kuba ngaphezu kwe-1.00%.
2.3 Isinyithi esinzima: Ukumiselwa ngokomthetho (People's Republic of China Pharmacopoeia 2010 Edition, Part II Appendix ⅧH) Ukumiselwa ngendlela yesibini.
Ukuchaneka ubunzima be-1.0g yemveliso yovavanyo, ukutshisa ngokukhawuleza kude kube yi-carbonized ngokupheleleyo, ipholile, yongeza i-0.5-1.0ml sulfuric acid, yenza ukuba ifumile, ishushu kwiqondo lokushisa eliphantsi kude kube yilapho i-asidi ye-sulfuric iphelile, yongeza i-0.5ml nitric acid, i-steam yomile, de kube umphunga we-nitrogen oxide uphelile, upholile, ushushu kwi-500-600 ℃ ukuba i-carbonized ngokupheleleyo, ipholile, yongeza i-2ml i-hydrochloric acid, Emva kokumisa kwindawo yokuhlambela amanzi, yongeza i-15ml yamanzi, yehla isisombululo sovavanyo lwe-ammonia de ibe yinto engathathi hlangothi kwisalathisi se-phenolphthalein. isisombululo, yongeza i-2ml i-acetate buffer (ph3.5), kunye nobushushu obuncinci buyinyibilike, yihambise kwi-tube ye-Nachner colorimetric, kwaye udibanise kwi-25ml ngamanzi.Thatha enye i-reagent yokulungiselela isisombululo sokuvavanya, kwaye uyifake kwisitya se-porcelain, yongeza i-2ml ye-acetate buffer (PH3.5) kunye ne-15ml yamanzi ekutshiseni kancinci Emva kokuchithwa, hambisa i-Nath colorimetric tube, yongeza inani elithile lesisombululo esiqhelekileyo sokukhokelela, kwaye emva koko uhlambulule ngamanzi ukuya kwi-25ml.Uvavanyo lwe-colorimetric lwenziwa phakathi kwesisombululo sovavanyo kunye nesisombululo esiqhelekileyo sokufumana.Ukulungiswa kwesisombululo esisemgangathweni ngokwe (People's Republic of China Pharmacopoeia 2010 edition II Isihlomelo Ⅷ indlela yokuvavanya isinyithi esinzima) indlela yokuqala.Isinyithi esinzima akufuneki sibe ngaphezu kweengxenye ezingama-20 kwisigidi ngasinye.
3. Ubunyulu: Ngokokusebenza okuphezulu kwechromatography yolwelo, emiselwe ngokomthetho (Chinese Pharmacopoeia 2010 edition II Appendix VD).
Iimeko zeChromatographic:
Ikholamu: C18, 200mm×4.6mm, 5μm;
Isigaba seselula: I-Phosphate buffer (ubunzima be-2.72g potassium dihydrogen phosphate, yongeza amanzi ukuze udibanise kwaye udibanise kwi-1000ml, lungisa i-pH = 3.5): i-acetonitrile: = 35:65;
Ukubona ubude bamaza: 254nm;
Izinga lokuhamba: 1.0ml / min.
Indlela yokumisela: Thatha malunga ne-30mg yale mveliso, yilinganise ngokuchanekileyo, yihlambulule kunye nesigaba esihambahambayo ukwenza uxinaniso malunga ne-0.3mg / ml, thatha i-20μl kwi-chromatograph yolwelo, urekhode ichromatogram.Ngokwendlela yokulinganisa indawo, ukucoceka akukho ngaphantsi kwe-99.0%.
Ukuthenga njani?Nceda uqhagamshelaneDr. Alvin Huang: sales@ruifuchem.com or alvin@ruifuchem.com
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I-2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-enye (CAS: 224789-21-3) yindawo ephakathi IVardenafil (CAS: 224785-90-4) / Vardenafil Hydrochloride (CAS: 224785-91-5).I-Vardenafil yi-PDE5 inhibitor entsha eqaliswe kunyango lomlomo lwe-erectile dysfunction yamadoda kwaye inokufana okuphawulekayo kwesakhiwo kunye ne-sildenafil (i-Viagra), eyayiyi-PDE5 inhibitor yokuqala eyaziswa kwi-1998 kwesi sibonakaliso.
I-Vardenafil yayiyi-arhente yesibini ukuba ithengiswe kwaye yayinenzuzo yokuba ixesha layo lokuqala alizange lincitshiswe ngokuthatha iyeza kwisisu esipheleleyo .Ngamaxesha e-30 anamandla njenge-inhibitor ye-PDE5 (ithetha i-IC50, i-3.9 nM) kune-sildenafil kunye namaxesha e-10 anamandla ngaphezu kwe-tadalafil, ngokukhetha okukhulu (> amaxesha angama-1,000) kwi-PDE5 yabantu kune-PDE2 yabantu, i-PDE3, kunye ne-PDE4 kunye ukhetho oluphakathi (> amaxesha angama-80) kwi-PDE1.I-PDE inhibitory selectivity kunye ne-in vitro kunye ne-vivo potency ye-PDE5 inhibitor vardenafil entsha.I-Vardenafil inqande ngokukodwa i-hydrolysis ye-cGMP nge-PDE5, kunye ne-IC50 ye-0.7 nM (sildenafil 6.6 nM).I-IC50 ye-vardenafil ye-PDE1 yayingu-180 nM, ye-PDE6 11 nM, kunye ne-PDE2, i-PDE3 kunye ne-PDE4 ngaphezu kwe-1,000 nM.