176961-13-0

Basic information

• Product Name: Boronic acid, [2-[[(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino]sulfonyl] phenyl]-
• CAS NO: 176961-13-0
• Molecular Formula: C15H21BN2O7S
• Molecular Weight: 384.218
• Mol File: 176961-13-0.mol

Chemical Properties

• CAS DataBase Reference: Boronic acid, [2-[[(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino]sulfonyl] phenyl]-(CAS DataBase Reference)
• NIST Chemistry Reference: Boronic acid, [2-[[(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino]sulfonyl] phenyl]-(176961-13-0)
• EPA Substance Registry System: Boronic acid, [2-[[(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino]sulfonyl] phenyl]-(176961-13-0)

Safety Data

• Hazardous Substances Data: 176961-13-0(Hazardous Substances Data)

Upstream product

• 19947-75-2 5-amino-3,4-dimethylisoxazol 
• 2905-25-1 o-bromobenzenesulfonyl chloride 
• 121-43-7 Trimethyl borate 
• 153624-30-7 2-bromo-N-(3,4-dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]benzenesulfonamide 
• 688-74-4 boric acid tributyl ester 
• 98-09-9 benzenesulfonyl chloride 
• 153623-86-0 N-(3,4-Dimethyl-5-isoxazolyl)-2-bromo-benzenesulfonamide 

Downstream Products

• 176961-19-6 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(4-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-14-1 N-(3,4-dimethyl-5-isoxazolyl)-N-[(methoxyethoxy)methyl]-4'-(2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-21-0 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(4-methyl-2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-22-1 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(5-methyl-2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-34-5 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(2-oxazolylmethyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-17-4 N-(3,4-Dimethyl-5-isoxazolyl)-4'-(4,5-dimethyl-2-oxazolyl)-N-[(2-methoxyethoxy)methyl][1,1'-biphenyl]-2-sulfonamide 
• 181133-18-6 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(2-pyridinyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-35-6 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(5-isoxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-15-2 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(2-thiazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 197074-72-9 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(1,3,4-oxadiazol-2-yl)[1,1'-biphenyl]-2-sulfonamide 
• 181133-19-7 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(3-pyridinyl)[1,1'-biphenyl]-2-sulfonamide 
• 181133-22-2 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(4-pyrimidinyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-23-2 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(1H-pyrazol-1-yl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-26-5 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(1-methyl-1H-imidazole-2-yl)[1,1'-biphenyl]-2-sulfonamide 

Relevant articles and documents

Novel method for cheaply and efficiently synthesizing 2-dihydroxyboro-N-dimethylisooxazolyl-N-methoxyethoxymethyl benzsulfamide

The invention relates to a novel method for cheaply and efficiently synthesizing 2-dihydroxyboro-N-dimethylisooxazolyl-N-methoxyethoxymethyl benzsulfamide. The full name of the 2-dihydroxyboro-N-dimethylisooxazolyl-N-methoxyethoxymethyl benzsulfamide is 2

Synthesis and biological evaluation of 4′-[(benzimidazole-1-yl) methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists

A series of 4′-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives (Ia-Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT1 and endothelin ETA receptors (AT1 IC50 = 8.5, ETA IC50 = 8.9 nM), and was more potent than losartan in RHRs with no significant effect on heart rate. The preliminary structure-activity relationships were also discussed in the present paper.

Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.

A series of 4'-[(imidazol-1-yl)methyl]biphenylsulfonamides has potent antagonist activity against both angiotensin II AT(1) and endothelin ET(A) receptors. Such dual-acting antagonists could have utility in the treatment of hypertension, heart failure, an

Substituted biphenylsulfonamide endothelin antagonists

Compounds of the formula inhibit the activity of endothelin. The symbols are defined as follows: R2 and R3 are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) -C(O)H or -C(O)R6; (h) -CO2H or -CO2R6; (i) -SH, -S(O)nR6, -S(O)m-OH, -S(O)m-OR6, -O-S(O)m-R6, -O-S(O)mOH or -O-S(O)m-OR6; (j) -Z4-NR7R8; or (k) -Z4-N(R11)-Z5-NR9R10; and the remaining symbols are as defined in the specification.

HETEROARYL SUBSTITUTED PHENYL ISOXAZOLE SULFONAMIDE ENDOTHELIN ANTAGONISTS

Compounds of the formula STR1 inhibit the activity of endothelin.

N-Isoxazolyl-biphenylsulfonamide derivatives, their preparation and their use as endothelin antagonists

A compound of the formula I an enantiomer, diastereomer or pharmaceutically acceptable salt thereof, wherein: one of X and Y is N and the other is O; R2,R3,R4 and R5 are each independently (a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g)-C(O)H or-C(O)R6;(h)-CO2H or-CO2R6;(i)-SH,-S(O)nR6 ,-S(O)m-OH,-S(O)m-OR6,-O-S(O)m-R6,-O-S(O)mOH or-O-S(O)m-OR6;(j)-Z4-NR7R8; or(k)-Z4-N(R11)-Z5-NR9 R10; R4 and R5 together are alkylene or alkenylene, either of which may be substituted with Z1,Z2 and Z3, completing a 4-to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; G1 is (a) hydrogen; or(b) alkyl; G2 is (a) hydroxyalkyl;(b)-(CH2)mOR6; or(c)-(CH2)m-NR12 R13;(d) mono-to hexa-halo substituted alkyl; or(e)-(CH2)n OR14; and the remaining symbols are as defined in the description.The compounds of formula I are antagonists of ET-1, ET-2 and /or ET-3 and are useful in treatment of conditions associated with increased ET levels (e.g., dialysis, trauma and surgery) and of all endothelin-dependent disorders. They are thus inter alia useful as antihypertensive agents.