Category «Uncategorized»

(Z)-3-Chloro-3-(3′-fluorophenyl)-acrylonitrile

It’s only fair to share… cas 1192875-03-8, 181.59 C9 H5 Cl F N 2-Propenenitrile, 3-chloro-3-(3-fluorophenyl)-, (2Z)- WO 2009133389 IV V VI II Example 1: Synthesis of (Z)-3-Chloro-3-(3-fluorophenyl)-acrylonitrile from 3′-Fluoroacetophenone. To a solution of 3′-fluoroacetophenone (80.0 g, 0.579 mol) in 7V,N-dimethyl formamide (560 ml) at about 400C was added phosphoryl chloride (92.50 ml, 1.01 mol) dropwise, maintaining …

AZD 7762

It’s only fair to share… AZD7762 CAS 860352-01-8 AZD7762; 860352-01-8; AZD-7762; AZD 7762; (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; UNII-5D822Y3L1H 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide Potent and selective ATP-competitive inhibitor of Chk1 and Chk2 (IC50 vales are 5 nM for both kinases); displays at least >10 fold selectivity over a panel of 164 kinases. Potentiates cytotoxicity of DNA-damaging agents HCL; SALT, Technical Data M.Wt:398.88, Formula:C17H19FN4O2S.HCl Solubility:Soluble …

Lorlatinib, лорлатиниб , لورلاتينيب , 洛拉替尼 , PF-6463922

It’s only fair to share… Lorlatinib, PF-6463922 For Cancer; Non-small-cell lung cancer Molecular Formula C21H19FN6O2 Average mass 406.413 Da Phase 2 WO 2013132376 Andrew James Jensen, Suman Luthra, Paul Francis RICHARDSON Applicant Pfizer Inc. (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-4,8- methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile (16R)-19-Amino-13-fluoro-4,8,16-trimethyl-9-oxo-17-oxa-4,5,8,20-tetraazatetracyclo[16.3.1.02,6.010,15]docosa-1(22),2,5,10,12,14,18,20-octaene-3-carbonitrile (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile CAS 1454846-35-5 [RN] UNII:OSP71S83EU лорлатиниб [Russian] لورلاتينيب [Arabic] 洛拉替尼 [Chinese] Ros1 tyrosine kinase receptor inhibitor; Anaplastic lymphoma kinase receptor inhibitor useful …

(l,4-bis((3-(l-propylpiperidin-4′ yl)phenyI)sulfonyl)butane)

It’s only fair to share…   Example 3 – Preparation Of Compound 3 (l,4-bis((3-(l-propylpiperidin-4′ yl)phenyI)sulfonyl)butane) Preparation of 1.4-bis((3-bromophenyl)thio‘)butane (Compound 3. 1st int.) 1 ,4-bis((3-bromophenyl)thio)butane KOH (56.2g) was added into methanol (1200mL) in 15min. The clear solution was cooled on water bath to 0°C. A solution of 3-bromo thiophenol (150.2g, 0.79mol) in methanol (200mL) was added …

(4-(3-(methylsulfinyl)phenyl)-l-propyl-l,2,3,6- tetrahydropyridine)

It’s only fair to share… Example 7 – Preparation Of Compound 7 (4-(3-(methylsulfinyl)phenyl)-l-propyl-l,2,3,6- tetrahydropyridine) 4-(3-(methylsulfinyl)phenyl)-1-propyl- 1 ,2,3,6-tetrahydropyridin-1-ium chloride Sulfuric acid (42.23g, 0.43 lmol, leq) was added to a mixture of 4-hydroxy-4-(3- (methylsulfonyl)phenyl)-l-propylpiperidin-l-ium chloride (130g, 0.431 mo, leq) and toluene (650mL) at room temperature. The resulting two-phase solution was refluxed for lhour and HPLC showed that …

(l-(3,3-bis(3-(methylsulfonyI)phenyl)propyl)-4-(3- (methylsulfonyl) phenyl)piperidine)

It’s only fair to share…   Example 2 – Preparation Of Compound 2 (l-(3,3-bis(3-(methylsulfonyI)phenyl)propyl)-4-(3- (methylsulfonyl) phenyl)piperidine) Preparation of ethyl 3-(4-oxopiperidin-l-yl)-propanoate (starting material for Compound 2) 3-(4-oxopiperidin-1-yl)-propanoate Ethanol (1550mL) was poured into a 4 L three-necked round-bottom flask equipped with over-head stirring followed by the addition of 125g (814mmol, leq) 4-piperidone monohydrate hydrochloride and 225g (1628mmol, …

((3R,4S)-4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-3-ol)

It’s only fair to share… Example 4 – Preparation Of Compound 4 ((3R,4S)-4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-3-ol) Preparation of dS,6S)-6-(3-(methylsulfonvnphenyl)-3-propyl-7-oxa-3-azabicyclo [4.1.Olheptane (1S,6S)-6-(3-(methylsulfonyl)p enyl) -3-propyl-7-oxa-3-azabicyclo [4.1.0]heptane Into a 4L reactor was added at room temperature Compound 8 (229g, 820mmol, leq) and 2N sulfuric acid (1147mL, 112g sulfuric acid, 1.147mol, 1.4eq). The reaction light yellow mixture was stirred and sodium bromate …

(l-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine)

It’s only fair to share… Example 6 – Preparation Of Compound (l-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine) 1-(2-methylpentyl)-4-(3- (methylsulfonyl)phenyl)piperidine Into a 1L autoclave was added KI (28.4g, 171mmol leq) and potassium carbonate (47.4g, 343mmol, 2eq). 4-(3-(methylsulfonyl)phenyl)piperidine (41g, 171mmol, leq) was dissolved in acetonitrile (420mL) and the mixture was added into the autoclave followed by l-chloro-2-methylpentane (25.8mL, 188mmol, l .leq). The …

New Website goflow.at online! from C. Oliver Kappe, University of Graz

It’s only fair to share… New Website goflow.at online! C. Oliver Kappe Professor at University of Graz Institute of Chemistry Univ.-Prof. Mag. Dr.rer.nat. +43 316 380-5352 +43 (0) 316 380 – 9840 Oliver.kappe (at) uni-graz.at Research in the Kappe lab focuses on flow chemistry, microreactor technology, process intensification and the continuous generation of active pharmaceutical ingredients …

Darifenacin Hydrobromide, 臭化水素酸ダリフェナシン

It’s only fair to share…   Darifenacin 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide Darifenacin; Emselex; Enablex; CAS 133099-04-4; UNII-APG9819VLM; US 2004-12-22 APPROVED EU 2004-10-22 APPROVED Molecular Formula: C28H30N2O2 Molecular Weight: 426.56 g/mol Title: Darifenacin CAS Registry Number: 133099-04-4 CAS Name: (3S)-1-[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-a,a-diphenyl-3-pyrrolidineacetamide Additional Names: 3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]pyrrolidine; (S)-2-[1-[2-(2,3,-dihydrobenzfuran-5-yl)ethyl]-3-pyrrolidinyl]-2,2-diphenylacetamide Manufacturers’ Codes: UK-88525 Molecular Formula: C28H30N2O2 Molecular Weight: 426.55 Percent Composition: C 78.84%, H 7.09%, N 6.57%, O …