Hauj lwm lawm

Kev tsis

Lub hauv paus rau phau ntawv

raws

product-1400-1400

Cov khoom lag luam

### Systemtic Qhia Txog Ntawm Letrozole Cov Hmoov Hmoov

Letrozole yog qhov ua tau zoo tsis yog-steroidal aromatase inhibase, siv dav hauv kev kho mob cancer mis. Ua ib tus sawv cev ntawm cov tshuaj thib peb ntawm cov neeg ua haujlwm thib peb-aws Kab lus no yuav siv cov ntaub ntawv tseem ceeb ntawm cov khoom siv raw daws, cov txheej txheem tsim khoom, cov txheej txheem tsim khoom, kev tswj hwm zoo, kev nyab xeeb thiab kev nyab xeeb.

### 1. Tshuaj lom neeg thiab cov ntaub ntawv yooj yim

#### 1. Tshuaj lom neeg lub npe thiab cov qauv

- ** Lub npe tshuaj **: 4,4 '- (1h -1} {{-1- ylmethylene) Dibenzonitrile

- ** Molecular cov mis **: C17H11N5

- ** Molecular hnyav **: 285.31 g / mol

- ** tus lej lej **: 112809-51-5

- ** Ob tus qauv mis **: 1,2, {3}} lub nplhaib zoo li cov tub ntxhais, ob lub paraanophleny los ntawm methylene. Lub xub ntiag ntawm lub nplhaib triazole yog cov qauv tseem ceeb tshwj xeeb ntawm nws cov kev xaiv siab.

### 2. Lub zog lub cev

- ** Pom zoo ** ** Dawb rau off-dawb crystalline hmoov

- ** Melting point **: Txog 181-184 degree

- ** Solubility **: soluble hauv cov kuab tshuaj organic (xws li methanol), soluble me ntsis hauv dej (txog}. 1 mg / ml hauv ph 7).

- ** STABLY **: ruaj khov nyob rau hauv cov xwm txheej qhuav thiab tsaus nti, tab sis rhiab rau cov muaj zog acids thiab muaj zog oxidants.

#### 3. Tshuaj lom neeg

- ** Acid-puag zog **: Tsis muaj neeg Alkaline (Nitrogen atoms (Nitrogen atoms hauv lub nplhaib triazole tuaj yeem khi cov protons).

- ** Revelity Age ** CYANOPHENYL tus qauv muab nws cov hluav taws xob thiab tuaj yeem koom nrog kev hws lossis kev sib cav sib ceg.

- ** Cov hluavtaws nruab nrab ntawm nruab nrab **: feem ntau siv cov intermediates suav nrog 4-, 4- triazole sodium ntsev.

### 2. Lub chaw muag tshuaj thiab chaw kuaj mob zoo

### 1. Mechanism ntawm kev ua

- ** SHOMATIVE Inhibition **: Los ntawm kev sib tw sib tw rau Hemne Pawg ntawm Cytochrome ua haujlwm thiab thaiv kev hloov dua siab tshiab ntawm androstenione) rau Estrogens (Estradiaol).

- ** Xaiv tau **: Tsis muaj cov cuam tshuam tseem ceeb ntawm synthesis ntawm adrenal cortical cov tshuaj hormones, txo cov kev mob tshwm sim.

#### 2. Pharmacokinetics

- ** Rho Tawm **: Qhov ncauj Bioavailability yog 99.9%, thiab khoom noj tsis muaj qhov cuam tshuam tseem ceeb ntawm kev nqus.

- ** TSEG TSHWJ XEEB **: Cov tshuaj tiv thaiv protein khi muaj txiaj ntsig yog li 60%, thiab nws yog dav faib rau hauv cov ntaub so ntswg.

- ** Metabolism "feem ntau yog metabolized mus rau unactive carboxylic acid metabolites los ntawm daim siab cyp3A4 / CYP2A6.

- ** ** Ib nrab-lub neej **: Txog 2 hnub, txhawb nqa ib zaug noj tshuaj.

#### 3. Kev kuaj mob zoo

- ** High Efficiency **: Rau cov neeg mob cancerpauality cancer mis, nws tuaj yeem txo qib cov qib tshuaj estrogen los ntawm {1}}%.

- ** QUB Hla-Reverance **: Tsis muaj tus ntoo khaub lig-resistance nrog tamoxifen, haum rau kev kho kab ob kab.

- ** TSHOOJ TSHUAJ TIV THAIV ** Cov tshuaj kho mob tsoosietapy tsoosothery, cov nyom tshwm sim (xws li mob kub thiab mob pob txha) yog qhov me me.

### 3. Cov txheej txheem ntau lawm thiab thev naus laus zis thev naus laus zis

### 1. Synthesis txoj kev

- ** Txoj kev classic **:

1. Kev ua hws ntawm 4- bromomethylbluylentry thiab 1h 4-}}} pa solvent (xws li DMF).

2. Kev ua kom huv ntawm cov nruab nrab (crystallization lossis kem chromatography).

3. Kom qhuav thiab tsoo ntawm cov khoom kawg.

- ** Ua kom ua kom tau zoo dua **: Nce cov tshuaj tiv thaiv kev ua tau zoo rau ntau dua 85% los ntawm catalysts (xws li theem hloov catalysts).

#### 2. Cov teeb meem kev sib tw

- ** ORGURED tswj **: Nws yog qhov tsim nyog los saib xyuas cov khoom lag luam (xws li ob npaug rau cov khoom lag luam) thiab cov kuab tshuaj uas tseem tshuav (dmf, thf).

- ** Kev txhim kho ntsuab ntsuab ** Siv cov tshuaj tiv thaiv theem lossis microwave-pab synthesis los txo kev siv cov organic cov kuab tshuaj.

#### 3. Crystallization txheej txheem

- ** Kev tshawb nrhiav polymorphism **: Muaj ob lub crystal cov ntawv (hom uas ruaj khov, thiab qib siab yuav tsum tau txais los ntawm kev tswj hwm cov kuab tshuaj (xws li Eethanol / Dej System).

### 4. Daim Ntawv Thov Cov Lus Qhia thiab Taw Qhia

#### 1. Kev kho mob cancer mis

- ** Kev kho tus yam ntxwv zoo

- ** Metastatic mis cancer **: Cov kev ua kom muaj txiaj ntsig nruab nrab-dawb muaj txoj sia nyob ntawm thawj-kab kev kho yog {3}} lub hlis.

### 2. Lwm cov ntawv thov yuav

- ** Qis ntxiv lawm tshob **: Kev siv tshuaj tsawg yog siv los ua ovulation (tawm-daim ntawv lo, kev sib cav).

- ** Cov kev tshawb fawb kab mob estrogen-basen-basen-entent

### 5. Tswjhwm thiab cov qauv

### 1. Nrhiav txoj kev

- ** HPLC txujci **: C18 kem, mobile theem yog acetonitrile-phosphate tsis, nrhiav kev yoj yog 240 nm.

- ** Pib cov qauv kev xav tsis meej **: Yuav tsum ntsib Ich Q3A cov qauv, tag nrho cov impurities tsawg dua los yog sib npaug {2}}. 5%.

- ** Nco ntsoov tias tsis muaj enantiomers (tsis muaj chiral center yog koom nrog hauv synthesis txoj kev).

#### 2. Kev kawm ruaj khov

- ** Kev ntsuas kev nrawm **: 6 hlis ntawm 40 degree / 75% RH, cov ntsiab lus hloov yuav tsum yog tsawg dua lossis sib npaug rau 2%.

- ** ** Lub sijhawm ntev cia **: Nws raug pom zoo rau khw hauv qab 25 degree deb ntawm lub teeb, nrog lub neej txee ntawm 3 xyoos.

### 6. Kev ua lag luam cov xwm txheej thiab kev sib tw toj roob hauv pes

#### 1. Kev ua lag luam loj

- ** Qog thoob ntiaj teb no **: Kev lag luam loj hauv 2023 yog hais txog US $ 850 lab, nrog ib xyoos kev loj hlob txhua xyoo ntawm 6%.

- ** Kev faib tawm hauv cheeb tsam **: North America cov nyiaj rau 45%, Europe 30%, thiab Asia-Pacific cheeb tsam loj hlob sai (Tuam Tshoj Accials rau 50% ntawm Asia-Pacific Share).

#### 2. Cov tuam txhab loj

- ** Cov chaw tsim tshuaj paus qub **: Novartis (lub npe lag luam femara), daim patent tau tas sijhawm.

- ** Cov tuam txhab siv tshuaj General **: Is Nrias teb Lub Hnub Ci Tshuaj, Tuam Tshoj lub tshuaj loog Hengru, nws cov tshuaj his raprgineutical, thiab lwm yam.

#### 3. Tus Nqi

- ** Nqe ntawm API **: Tus nqi nruab nrab hauv 2023 yog li $ 2500 / kg, ib 20% txo ntawm 2019 (vim kev sib tw los ntawm cov tshuaj tsis muaj zog).

### 7. Kev Nyab Xeeb thiab Kev Cai Tswjfwm

#### 1. Cov ntaub ntawv lom zem

- **Acute toxicity**: Oral LD50 in rats>2000 mg / kg (qis ncu toxicity).

- ** ** Lub sijhawm ntev kev sim siab **: Kev sim tsiaj qhia tias cov koob tshuaj muaj txiaj ntsig ntau yuav ua rau lub siab ua kom haum.

#### 2. Sab txiaj ntsig kev tswj hwm

- ** ** OB TXHUA YAM RAWS LI CAS **: Cov Flash Kub (30%), mob sib koom tes (25%).

- ** Kev pheej hmoo loj **: Osteoporosis (calsteoporosis (calcium thiab vitamin d ntxiv ntxiv).

#### 3. Kev tswj txoj cai ua raws

- ** GMP daim ntawv pov thawj **: Yuav tsum ua raws li FDA 21 CFR Tshooj 211 lossis EU GMP Annex 2.

- ** Ib puag ncig yuav tsum tau ua rau ib puag ncig ": cyanide tsim thaum saptthesis yuav tsum ua nruj me ntsis (xws li sodium hypochlorite oxidation).

### 8. Yav Tom Ntej Kev Txhim Kho thiab Tshawb Fawb

1. ** Kev tsim kho cov qauv tshiab **: xws li kev txhaj tshuaj tiv thaiv ntev thiab ua rau thaj ua kom zoo dua los txhim kho tus neeg mob ua raws.

2. ** Kev tshawb nrhiav ntawm kev sib xyaw ua ke **: ua ke nrog CDK4 / 6 Inhibitors (xws li PalbocicLib) los txhim kho kev ua tau zoo.

3. ** Daim ntawv thov ntawm cov hluavtaws biology **: Siv cov khoom siv uas tsim kho kom raug cov nqi nruab nrab kom txo cov nqi tsim khoom.

### cov ntsiab lus

Vim nws cov txheej txheem siab, cov txheej txheem zoo nkauj thiab cov txheej txheem ua pov thawj, Letrozole API tau dhau los ua ib qho ntawm cov tshuaj tseem ceeb rau kev kho mob cancer mis. Nrog rau kev ua kom zoo ntawm cov txheej txheem ntau lawm thiab kev nthuav dav ntawm kev qhia tshiab, nws txoj haujlwm hauv kev lag luam hauv ntiaj teb yuav txuas ntxiv ua ke. Yav tom ntej, kev sib xyaw ua ke ntawm ntsuab synthesis thiab cov tshuaj nplig yuav txhawb nws txoj kev loj hlob.