Dab tsi yog qhov kev tshawb fawb tshiab ntawm kev tsim cov tshuaj sitagliptin phosphate?

Sitagliptin Phosphate yog dipeptidyl peptidase-4 (DPP-4) inhibitor siv los kho mob ntshav qab zib hom 2. Nws tau tsim los ntawm MSD thiab pom zoo rau kev lag luam hauv Tebchaws Meskas hauv xyoo 2006. Raws li thawj DPP-4 inhibitor tshuaj, nws nce qib glucagon zoo li peptide-1 (GLP-1) hauv lub cev los ntawm inhibiting DPP-4 enzyme kev ua, yog li txhim kho insulin secretion thiab txo glucagon ntau lawm, tswj cov ntshav qabzib concentration. Vim nws txoj kev ua tau zoo heev thiab cov kev mob tshwm sim tsawg,Sitagliptin Phosphate hmoov sai sai tau los ua ib qho ntawm cov tshuaj tiv thaiv mob ntshav qab zib tau siv dav thoob ntiaj teb

Dab tsi yog cov txheej txheem tsim khoom thiab kev ua haujlwm ntawm Sitagliptin Phosphate API hmoov ??

Kev tsim cov txheej txheem ntawm sitagliptin phosphate feem ntau suav nrog cov tshuaj synthesis thiab tshuaj enzymatic synthesis. Txoj kev siv tshuaj lom neeg feem ntau siv 2,4,5-trifluorophenylalanine acid ua cov khoom pib, thiab cov khoom lag luam tau txais los ntawm kev sib xyaw ua ke, decarboxylation, asymmetric txo, amidation, deprotection thiab phosphoric acid salification, nrog rau tag nrho cov txiaj ntsig ntawm kwv yees li 33%. Txoj kev no muaj cov kauj ruam ntev, tab sis cov kev mob tshwm sim yog me me thiab stereoselectivity yog qhov zoo, yog li nws muaj kev lag luam zoo rau kev thov.
Chemical enzymatic synthesis siv diketone intermediate li raw khoom, thiab reacts nrog yooj yim chemical intermediate los tsim sitagliptin nyob rau hauv lub catalysis ntawm immobilized enzyme, thiab ces tsim ntsev nrog dilute phosphoric acid los npaj.sitagliptin phosphate monohydrate api hmoov. Cov txheej txheem muaj qhov zoo ntawm kev ua haujlwm yooj yim, mob me me, siab purity thiab cov txiaj ntsig zoo, thiab yog qhov tsim nyog rau kev tsim khoom loj -.
Hauv kev tsim khoom,peb lub tuam txhabfeem ntau yog ua los ntawm cov tshuaj enzymatic txoj kev, thiab cov kauj ruam tseem ceeb muaj xws li condensation khoom synthesis, R- chiral txo cov khoom synthesis, hydrolysis khoom synthesis thiab hais txog. Cov khoom nruab nrab tau tsim los ntawm condensation, alcoholysis, ammonolysis, hydrolysis, Boc tiv thaiv, deprotection, salification thiab lwm yam tshuaj, thiab ces refined los ntawm centrifugation, ntxuav, centrifugation, ziab thiab lwm yam txheej txheem. Kev tsim tawm ntawm sitagliptin phosphate tuaj yeem ncav cuag ntau dua 99%, uas ua tau raws li daim ntawv thov ntawm cov chaw tsim tshuaj.

Dab tsi yog qhov kev tshawb fawb tshiab ntawm kev tsim cov tshuaj sitagliptin phosphate?

Cov kev tshawb fawb tshiab kawg ntawm kev tsim cov sitagliptin phosphate tsuas yog tsom rau cov txheej txheem ntsuab synthesis, kev tswj tsis huv tseem ceeb, kev tsim khoom tas li thiab cov kev qhia tshiab nthuav dav.

Ua ntej. Optimization ntawm ntsuab synthesis txheej txheem

Enzymatic txoj kev:Txoj kev ntsuab ntawm synthesizing sitagliptin catalyzed los ntawm ω-transaminase (xws li ATA117) tau dhau los ua qhov tseem ceeb. Los ntawm optimizing thev naus laus zis ntawm enzyme immobilization, cov tshuaj tiv thaiv nruab nrab thiab cov khoom sib cais, txoj hauv kev muaj kev lag luam siab atomic thiab dej khib nyiab tsawg, thiab tag nrho cov txiaj ntsig tuaj yeem ncav cuag 76%. Cov tuam txhab lag luam hauv tsev tau tsim immobilized transaminase (xws li SZ-0022E-IMMO-B) thiab ua lag luam. Los ntawm kev qhia transaminase nyob rau hauv recombinant Escherichia coli, lub substrate conversion tus nqi tuaj yeem ncav cuag 95.83%, qhov tawm los yog 84.6%, thiab tus nqi ee yog tshaj 99.99%.
Kev txhim kho ntawm chemical synthesis:los ntawm optimizing cov kauj ruam ntawm condensation, alcoholysis, ammonolysis, hydrolysis, Boc tiv thaiv, deprotection thiab salification, kev siv cov precious hlau catalyst yog txo, thiab cov hnyav rov qab system yog optimized kom txo tau lub zog noj thiab "peb pov tseg" emission. Piv txwv li, hloov cov tshuaj organic hnyav nrog cov kuab tshuaj sib xyaw ntawm DMF thiab dej tuaj yeem txo qis cov organic hnyav.

thib ob. Tswj thiab tsom xam cov txheej txheem ntawm impurities tseem ceeb

A. Nitrosamine impurity tswj:Nws tau pom tias NTTP tuaj yeem tsim tawm thaum lub sijhawm khaws cia ntawm sitagliptin phosphate, thiab huab cua raug yog qhov tseem ceeb. Los ntawm kev txhim kho cov ntaub ntawv ntim khoom (xws li cov khoom siv oxygen permeability tsawg) thiab cov xwm txheej cia, NTTP tsim tuaj yeem cuam tshuam zoo.
B.Dimer impurity tswj:Jiangsu Wichita Pharmaceutical Co., Ltd. tau tsim ib txoj hauv kev rau kev txiav txim siab ntawm cov ntsiab lus dimer impurity, uas txhim kho qhov rhiab heev thiab qhov tseeb ntawm kev tshawb nrhiav thiab pab cov lag luam kom tswj tau qhov zoo ntawm cov tshuaj ntau lawm.
Kev tswj tsis huv ntawm phosphate: UPLC-MS txoj kev tau tsim los txiav txim siab cov ntsiab lus ntawm trimethyl phosphate (TMP) thiab triisopropyl phosphate (TIP) hauv sitagliptin phosphate. Txoj kev no yog qhov yooj yim, ceev, rhiab thiab raug, thiab haum rau kev tshawb pom ntawm ultra- kab rov tav theem.
C.Impurity tswj ntawm nruab nrab:HPLC dual- txoj kev wavelength yog tsim los rau ib txhij txiav txim siab malonic acid nyob rau hauv nruab nrab ntawm sitagliptin phosphate. Txoj kev no muaj qhov tshwj xeeb muaj zog thiab raug siab, thiab tuaj yeem siv rau kev tswj xyuas qhov nruab nrab.

Peb. nruam ntws cov tshuaj tiv thaiv thiab ntse ntau lawm

I.Continuous flow reaction technology:Piv nrog rau cov tshuaj tiv thaiv kab mob ib txwm muaj, cov tshuaj tiv thaiv tsis tu ncua tuaj yeem txhim kho kev ua haujlwm tau zoo los ntawm 30% thiab txo kev siv hluav taws xob los ntawm 20%. Los ntawm kev qhia txog cov txheej txheem kev tshuaj ntsuam xyuas thev naus laus zis (PAT) thiab kev saib xyuas online, tiag tiag- lub sijhawm saib xyuas thiab tso tawm cov yam ntxwv tseem ceeb tuaj yeem ua tiav, lub voj voog ntau lawm tuaj yeem txo qis thiab kev ruaj ntseg zoo tuaj yeem txhim kho.
II.Intelligent ntau lawm:Los ntawm kev qhia AI, Is Taws Nem ntawm Yam thiab cov ntaub ntawv thev naus laus zis, tiag tiag - sijhawm saib xyuas thiab kev ua kom zoo ntawm cov txheej txheem tsim khoom tuaj yeem ua tiav. Cov kev tswj xyuas ntse tuaj yeem txhim kho cov khoom tsim tau los ntawm 25%, cov khoom tsim nyog tus nqi ntau dua 99.5%, thiab txo cov nqi zog.

Plaub: nthuav qhia tshiab

Kev tiv thaiv kev mob qog noj ntshav- tiv thaiv- tus kab mob (aGVHD): Ib qho -center theem II kev tshawb fawb soj ntsuam (CTR20254033) tab tom soj ntsuam kev ua tau zoo thiab kev nyab xeeb ntawm sitagliptin phosphate hauv kev tiv thaiv aGVHD hauv cov neeg mob uas tau txais cov ntshav allogeneic peripheral. Luv-lub sij hawm (4 zaug) thiab ntev- lub sij hawm (10 zaug) cov txheej txheem tswj hwm tau raug coj los siv hauv txoj kev tshawb no, uas tau muab lub hauv paus kho mob rau kev tsim cov kev qhia tshiab ntawmsitagliptin phosphate API hmoov.

Vim li cas thiaj xaiv peb lub tuam txhab cov khoom siv raw rau sitagliptin phosphate hmoov?

Piv nrog rau lwm lub tuam txhab,Xi'an Faithful BioTech Co., Ltd.muaj plaub qhov zoo: tus nqi thiab nplai, thev naus laus zis thiab zoo, xa tawm thiab ntawv pov thawj, txoj cai thiab kev ua lag luam. Hais txog tus nqi thiab nplai, peb ua tiav cov nqi coj noj coj ua los ntawm kev loj - kev tsim khoom thiab kev lag luam sib sau ua ke; Nyob rau hauv cov nqe lus ntawm technology thiab zoo, peb txais yuav ntsuab synthesis txoj kev thiab siv QbD tswvyim los xyuas kom meej tias cov impurity spectrum ntawm cov khoom yog zoo dua li EP / USP tus qauv; Hais txog kev xa tawm thiab ntawv pov thawj, peb muaj cov ntawv pov thawj thoob ntiaj teb xws li CEP ntawm European Union thiab DMF ntawm Tebchaws Meskas, thiab tau ntse nkag mus rau European thiab Asmeskas cov qauv kev lag luam; Hais txog txoj cai thiab kev ua lag luam, peb tau txais txiaj ntsig los ntawm kev hloov kho cov ntawv pov hwm kho mob hauv lub tebchaws thiab kev txhawb nqa ntawm "14th Tsib-Year Plan" txoj cai kev lag luam biomedical, thiab kev lag luam kev cia siab yog dav. Yog tias koj tuaj yeem muab cov ntaub ntawv tshwj xeeb txog koj lub tuam txhab, kuv tuaj yeem tsim cov ntawv tshaj tawm kev tsom xam kom zoo dua rau koj.

Yog tias koj txaus siab rau peb cov khoom, lossis muaj cov lus qhia tseem ceeb ntawm peb cov khoom lossis tsis txaus siab rau cov khoom tau txais, Thov hu rau peb ntawmEmail: sales6@faithfulbio.com; Peb pab neeg tau cog lus los ua kom tiav kev txaus siab ntawm cov neeg siv khoom.