69395-15-9

Usage

Appearance

White to light yellow crystalline solid

Usage

Pharmaceutical intermediate, antimicrobial and antifungal agent in medicinal and personal care products

Role

Building block in organic synthesis for creating complex compounds for pharmaceutical and industrial applications

Hazards

Toxic and hazardous substance, requires proper safety precautions during handling and storage.

Upstream product

• 350-30-1 3-chloro-4-fluoronitrobenzene 
• 73088-10-5 2-(2-chloro-4-nitro-phenyl)-malonic acid dimethyl ester 
• 73088-11-6 2-(2-chloro-4-nitrophenyl)acetic acid 
• 50-00-0 formaldehyd 
• 121-86-8 2-chloro-4-nitrotoluene 
• 103-45-7 acetic acid phenethyl ester 
• 104-30-3 2-(4-nitrophenyl)ethyl acetate 

Downstream Products

• 69497-21-8 (5'-O-Tritylthymidin-3')(2-chlorphenyl)(2-chlor-4-nitrophenylaethyl)phosphorsaeureester 
• 74712-82-6 Phosphoric acid 2-(2-chloro-4-nitro-phenyl)-ethyl ester 2,5-dichloro-phenyl ester (2R,3S,5R)-5-(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2-trityloxymethyl-tetrahydro-furan-3-yl ester 
• 79536-90-6 (5'-O-Trityl-thymidin-3')(2-chlor-4-nitrophenylaethyl)(p-nitrophenyl)phosphorsaeureester 
• 74706-79-9 Phosphoric acid 2-(2-chloro-4-nitro-phenyl)-ethyl ester 2,5-dichloro-phenyl ester (2R,3S,5R)-2-[(4-methoxy-phenyl)-diphenyl-methoxymethyl]-5-(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-tetrahydro-furan-3-yl ester 
• 344285-84-3 4-amino-2-chlorophenethyl alcohol 
• 1026652-81-2 2-chloro-1-(2-methoxymethoxy-ethyl)-4-nitro-benzene 
• 247074-05-1 3-chloro-4-[2-(methoxymethoxy)ethyl]aniline 
• 227467-66-5 ethyl N-[4-(2-bromoethyl)-3-chlorophenyl]aminoacetate 
• 344285-85-4 ethyl N-[3-chloro-4-(2-hydroxyethyl)phenyl]aminoacetate 
• 247074-07-3 ethyl 2-[[3-chloro-4-(2-hydroxyethyl)phenyl]amino]-2-methylpropionate 
• 227467-68-7 ethyl N-[4-(2-bromoethyl)-2,3-dichlorophenyl]aminoacetate 
• 227467-69-8 ethyl N-[4-(2-bromoethyl)-2,5-dichlorophenyl]aminoacetate 
• 1028271-87-5 (3-Chloro-4-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methyl-ethylamino]-ethyl}-phenylamino)-acetic acid ethyl ester 
• 247073-85-4 2-(3-Chloro-4-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methyl-ethylamino]-ethyl}-phenylamino)-2-methyl-propionic acid ethyl ester 

Relevant academic research and scientific papers

NEODEGRADER CONJUGATES

The present disclosure provides neoDegraders and neoDegraders conjugated to binding moieties. Also provided are compositions comprising the conjugates. The compounds and compositions are useful for treating a disease or condition, e.g., cancer, in a subject in need thereof.

POLYNUCLEOTIDE CONSTRUCTS HAVING DISULFIDE GROUPS

The invention features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components is attached to an internudeotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains one or more bulky groups proximal to the disulfide group. The invention also features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components (i) is attached to an internudeotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains at least 4 atoms in a chain between the disulfide linkage and the phosphorus atom of the internudeotide bridging group or the terminal group; and where the chain does not contain a phosphate, an amide, an ester, or an alkenylene. The invention also features methods of delivering a polynucleotide to a cell using the polynucleotide constructs of the invention.

POLYNUCLEOTIDE CONSTRUCTS HAVING BIOREVERSIBLE AND NON-BIOREVERSIBLE GROUPS

The invention features a hybridized polynucleotide construct containing a passenger strand, a guide strand loadable into a RISC complex, and (i) a 3'-terminal or an internucleotide non-bioreversible group in the guide strand; or (ii) a 5'-terminal, a 3'-terminal, or an internucleotide non-bioreversible group in the passenger strand, and a 5'-terminal, a 3'-terminal, or an internucleotide disulfide bioreversible group in the guide strand or the passenger strand. The invention also features methods of delivering a polynucleotide to a cell using the hybridized polynucleotide construct. The invention further features methods of reducing the expression of a polypeptide in a cell using the hybridized polynucleotide construct.

Pharmaceutically Active Pyrazine Derivatives

The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1): and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0

PHARMACEUTICALLY ACTIVE PYRAZINE DERIVATIVES

The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1) and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0 o

PHARMACEUTICAL COMPOUNDS

The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group -CH2CH2- which together with the said one carbon atom forms a cyclopropyl group; m is 1, 2, 3 or 4; n is 0 or 1; and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R13 as defined in the claims. The compounds are inhibitors of Chk-1 kinase and are active against cancers.

Nucleotide. XIV. Substituierte β-Phenylaethyl-Gruppen. Neue Schutzgruppen fuer Oligonucleotid-Synthesen nach dem Phosphorsaeuretriester-Verfahren

Various o- and p-substituted β-phenylethanols (2-10) have been synthesized and investigated as blocking groups in the phosphotriester approach.A large number of 5'-O-tritylated thymidine-3'-phosphotriesters (13-36) with two different phosphate protecting groups have been prepared, characterized, and studied according to their chemical stability and usefullness for oligonucleotide syntheses.The combination of a 5'-O-monomethoxytrityl- and a 3'-(2,5-dichlorophenyl, p-nitrophenylethyl)-phosphate function as in 18 turned out to possess optimal properties as a monomeric nucleotide building block due to the fact that these blocking groups can be quantitatively and selectively be removed without harming each other by trifluoroacetic acid in chloroform to 41, by oximate to 42, and by DBU to 43.The base-catalyzed removal of the monosubstituted phenylethyl groups by DBU or DBN respectively as well as the disubstituted phenylethyl groups by triethylamine in aprotic solvents is a β-elimination process leading to phosphodiesters without attack on the P-center.