Quetiapine Fumarate hmoov CAS 111974-72-2

Quetiapine fumarate hmoovyog dibenzothiazepine derivative. Nws tshwm sim raws li cov dawb mus tawm -dawb crystalline hmoov uas xyaum insoluble nyob rau hauv dej tab sis soluble nyob rau hauv glacial acetic acid. Cov tshuaj muaj qhov melting point ntawm 170{10}}174℃. Cov yam ntxwv tsis hnov ​​tsw thiab saj tsis zoo ua rau nws yooj yim dua los tuav thiab khaws cia, thaum tseem txo qhov kev pheej hmoo ntawm kev tsis meej pem nrog lwm yam tshuaj. Khaws kom deb ntawm oxidants thaum khaws cia. Thaum rov ua dua tshiab, nws raug nquahu kom yaj thiab sib tov rau hauv cov kuab tshuaj combustible hauv cov tshuaj incinerator uas muaj cov khoom siv tom qab combustion thiab ntxuav. Nws yog ib tiam tshiab ntawm cov tshuaj atypical psychotropic. Zeneca yog thawj zaug hauv tebchaws Askiv thaum Lub Kaum Ib Hlis 1997. Clinically siv los ua thawj kab tshuaj rau kev kho tus mob schizophrenia.

Quetiapine fumarate hmoovyog ib qho tshuaj atypical antipsychotic uas siv cov tshuaj kho mob los ntawm antagonizing dopamine receptors thiab 5-hydroxytryptamine receptors. Nws siv npog ntau yam ntawm cov kab mob hauv lub hlwb thiab txuas ntxiv mus rau kev kho mob ntxiv thiab kev siv tshwj xeeb scenario. Cov kev siv tshwj xeeb yog raws li hauv qab no:

Core Indications: Schizophrenia thiab Bipolar Disorder

 

1. Kev kho mob schizophrenia
Nws yog thawj zaug - cov tshuaj kho mob rau tus mob schizophrenia, uas muaj cov txiaj ntsig zoo rau ob qho tib si cov tsos mob zoo (xws li kev hnov ​​​​lus, kev xav tsis zoo, thiab kev xav tsis zoo) thiab cov tsos mob tsis zoo (xws li kev xav tsis txaus ntseeg thiab kev tshem tawm hauv zej zog). Nws cov txheej txheem ntawm kev txiav txim txo cov dopamine overactivity los ntawm thaiv cov dopamine D2 receptors, thaum antagonizing 5-HT2 receptors txhim kho cov tsos mob tsis zoo. Kev sim tshuaj ntsuam xyuas tau pom tias nws luv luv - lub sij hawm ua tau zoo yog piv rau cov tshuaj ib txwm siv xws li chlorpromazine thiab haloperidol, thiab kev siv mus ntev tsis ua rau muaj kev nce siab ntxiv ntawm prolactin, txo qhov kev pheej hmoo ntawm cov kab mob endocrine.

 

2. Kev tswj kev puas siab puas ntsws bipolar
Manic rov: Raws li lub siab lub ntsws stabilizer, nws tuaj yeem tswj tau cov tsos mob ntawm kev puas siab puas ntsws bipolar (xws li lub siab xav, kev xav tsis zoo, kev pw tsaug zog tsis zoo) los ntawm kev tswj hwm 5-HT2 thiab D2 receptors kom sib npaug ntawm kev xav hloov pauv.
Kev sib xyaw ua ke: Rau cov neeg mob uas muaj ob qho tib si manic thiab kev nyuaj siab, nws txoj kev tswj hwm ob txoj kev tuaj yeem txo cov kev xav tsis zoo thiab txo qhov kev pheej hmoo ntawm kev tua tus kheej.
Adjuvant therapy: Thaum siv ua ke nrog lithium ntsev los yog sodium valproate, nws tuaj yeem txhim kho kev ua tau zoo thiab txo lub sijhawm ntawm kev tawm tsam, tshwj xeeb tshaj yog rau cov mob refractory.

Adjuvant therapy: ncua rau kev nyuaj siab thiab lwm yam kev puas hlwb

 

1. Adjuvant kho kev nyuaj siab
Rau cov neeg mob uas muaj kev nyuaj siab nrog cov tsos mob ntawm kev puas siab puas ntsws xws li kev hnov ​​​​lus thiab kev xav tsis zoo, Ping tuaj yeem txhim kho cov txiaj ntsig ntawm cov tshuaj tiv thaiv kev ntxhov siab, txo kev ntxhov siab, kev xav tua tus kheej, thiab kev pw tsaug zog. Lub tshuab tuaj yeem koom nrog kev ua haujlwm ib nrab ntawm 5-HT1A receptors, txhim kho lub siab hloov pauv thiab kev paub txog kev ua haujlwm.

2. Cov teeb meem ntxhov siab vim thiab tom qab-Taumatic stress disorder (PTSD)
Cov tsos mob ntxhov siab: Los ntawm kev tswj hwm amygdala prefrontal cortex txoj hauv kev, kev ceeb toom ntau dhau thiab kev ntshai cov lus teb raug txo, txo cov tsos mob tseem ceeb ntawm kev ntxhov siab dav dav (GAD).

 

PTSD kev kho mob: Nws muaj kev txhim kho ntawm kev tshaj tawm - kev mob flashback, zam kev coj cwj pwm, thiab kev ceeb toom siab, tshwj xeeb tshaj yog haum rau cov teeb meem nyuaj nrog cov yam ntxwv ntawm kev puas siab puas ntsws.
3. Kev puas siab puas ntsws vim muaj kab mob ntawm lub cev
Quetiapine fumarate yog ib qho ntawm cov tshuaj nyiam rau cov tsos mob ntawm kev puas siab puas ntsws xws li kev hnov ​​​​lus, kev xav, thiab kev ntxhov siab hauv cov kab mob hauv lub cev xws li Parkinson's kab mob thiab mob stroke, vim nws tsis tshua muaj kev pheej hmoo ntawm cov tshuaj tiv thaiv extrapyramidal (EPS).

Daim ntawv thov tshwj xeeb scenario: Insomnia thiab kev tswj cov neeg mob laus

 

1. Kev kho mob ntawm Stubborn Insomnia
Tsawg koob tshuajquetiapine fumarate hmoov(25-100mg / hnub) tuaj yeem tsim cov teebmeem sedative los ntawm antagonizing histamine H1 receptors, txo lub sijhawm pw tsaug zog, thiab ntev pw tsaug zog ntev. Nws qhov txiaj ntsig yog nyob rau hauv nws qhov tsis muaj qhov tsis zoo thiab qhov cuam tshuam tsawg kawg ntawm kev pw tsaug zog, ua rau nws tsim nyog rau cov neeg mob uas ua siab ntev lossis nyob ntawm benzodiazepines.

 

2. Kev Tswj Xyuas Cov Neeg Laus Tsis Txaus Siab
Kev hloov koob tshuaj: Vim tias cov metabolism qeeb qeeb hauv cov neeg laus, thawj koob tshuaj yuav tsum tau txo qis rau 25mg / hnub thiab maj mam nce mus rau qhov koob tshuaj zoo (feem ntau 150-300mg / hnub) kom txo tau cov kev tsis zoo xws li hypotension thiab kiv taub hau.
Kev kho mob comorbidity: Rau cov neeg laus uas muaj kab mob plawv thiab ntshav qab zib mellitus, quetiapine fumarate tsis cuam tshuam rau cov ntshav lipid thiab ntshav qab zib, thiab nws txoj kev nyab xeeb zoo dua li cov tshuaj tiv thaiv kab mob.

Ntxiv dibenzo [b, f][1, 4] azathio-11-(10h) ketone thiab toluene rau cov tshuaj tiv thaiv lub khob, ntxiv sodium carbonate tov, txias cia, tso cov tshuaj Triphosgene yaj hauv toluene, khaws qhov kub ntawm 0℃rau 1 teev, nce qhov kub thiab txias rau 20 ~ 30℃thiab khaws qhov kub thiab txias rau 25 feeb ua ntej qhov kawg ntawm nitrogen. Tail gas nkag mus rau hauv lub tank nqus. Cais txheej dej, ntxuav cov toluene txheej ob zaug nrog dilute hydrochloric acid, thiab tom qab ntawd ntxuav nws ob zaug nrog dej. Siv cov txheej txheem toluene thiab qhuav nws nrog anhydrous sodium sulfate, lim cov desiccant kom tau txais cov tshuaj toluene ntawm cov khoom siv chlorinated, thiab ncaj qha nkag mus rau cov tshuaj tiv thaiv tom ntej . 200g (1.15mol) ntawm 1- (2-hydroxyethoxy) ethyl piperazine thiab cov khoom potassium carbonate tau ntxiv rau cov tshuaj toluene cov khoom uas muaj cov tshuaj chlorine ua ntej peb zaug. Tom qab txhua qhov pub mis, lawv tau rhaub thiab rov ua dua rau 8 teev, thiab cov tshuaj tiv thaiv refluxing tau ntev li 24 teev. Tom qab cov tshuaj tiv thaiv, nws raug txo kom sov hauv chav tsev, tov nrog dej kom yaj cov khoom, thiab cov txheej dej raug tshem tawm. Cov txheej txheej toluene yog ntxuav nrog dej ob zaug, qhuav nrog anhydrous sodium sulfate, lim tawm cov desiccant, thiab evaporated toluene hnyav nyob rau hauv lub siab txo kom tau quetiapine roj. Ntxiv cov ethanol rau quetiapine roj, do kom yaj, ntxiv fumaric acid, cua sov thiab reflux rau 1 teev, txo qhov kub rau crystallization, lim, thiab qhuav kom tau quetiapine semifumarate. Cov ntsiab lus yog 99.2% (HPLC), thiab tag nrho cov txiaj ntsig yog 81.2%.

• Ntxiv isopropanol thiab dej rau hauv No. 1 peb lub qhov ncauj lub raj mis, ntxiv mercaptosalicylic acid thiab o-chloronitrobenzene nyob rau hauv stirring, hloov nrog nitrogen, lub kaw lus yog turbid kua, thiab ces ntxiv cov tshuaj thiab dej npaj los ntawm sodium hydroxide thiab dej; refluxing cov tshuaj tiv thaiv rau 10-12h, TLC nrhiav tau sulfhydryl salicylic acid, txias rau 20-30℃tom qab cov tshuaj tiv thaiv, kho pH ＜ 1 nrog concentrated hydrochloric acid, nplawm crystallization, pom, ntxuav nrog dej thiab toluene raws li 2 zaug, thiab ziab nyob rau hauv kev txo qis kom tau txais 2- phenyl acid, captobenyl acid. molar tawm los ntawm 90% thiab purity ntawm 98.5%.
• Ntxiv 2- (2-nitrophenylmercapto) benzoic acid thiab dichloromethane rau hauv No. 2 peb lub qhov ncauj lub raj mis, tee dichlorosulfoxide, ua cov tshuaj tiv thaiv tshav kub, tig qhuav, dilute cov roj nrog dichloromethane, ntxiv n-[2- (2-hydroxyethoxy) ethyl] piperazine, triethomethane 3 lub qhov ncauj rau hauv lub raj mis, thiab tsis muaj dichloromethane. qhov kub thiab txias, tso cov dichloromethane diluent saum toj no rau hauv lub cev, hnov ​​mob hauv cov khaubncaws sab nraud povtseg, ntxuav cov txheej txheem organic nrog sodium carbonate thiab dej raws, tig qhuav kom tau piperazine condensate.
• Ua kom sov lub piperazine condensate thiab formic acid, ntxiv cov hmoov hlau, ua cov tshuaj tiv thaiv tshav kub, lim thiab qhuav cov formic acid tom qab cov khoom siv raw cov tshuaj tiv thaiv los ntawm TLC, ntxiv methylene chloride thiab dej, kho cov pH nrog sodium bicarbonate tov, cais cov khaubncaws sab nraud povtseg, extract nrog methylene chloride rau 3 zaug, muab cov organic khaubncaws sab nraud povtseg, spinpine molecules 2% thiab 0. purity ntawm 99.8%.
• Quetiapine thiab fumaric acid tau salted hauv methanol thiab qhuav kom tau quetiapine semi fumarate nrog molar yield ntawm 92.0% thiab purity.Quetiapine fumarate hmoovntawm 99.5%.

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