107786-36-7

Upstream product

• 70264-94-7 methyl 4-(bromomethyl)-3-methoxybenzoate 
• 6146-52-7 5-nitroindole 
• 74733-24-7 4-formyl-3-methoxybenzoic acid methyl ester 

Downstream Products

• 126502-40-7 4-(1-Allyl-5-nitro-1H-indol-3-ylmethyl)-3-methoxy-benzoic acid methyl ester 
• 107754-15-4 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)-benzoic acid methyl ester 
• 189807-79-2 4-[1-difluoromethyl-5-nitro-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester 
• 189807-75-8 4-[1-carbamoyl-5-nitro-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester 
• 189807-66-7 4-[1-(benzhydryl-carbamoyl)-5-nitro-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester 
• 107754-12-1 4-[5-(cyclopentyloxycarbonyl)amino-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester 
• 150320-29-9 Methyl 3-methoxy-4-(5-nitro-1-(7-chloroquinolin-2-ylmethyl)indol-3-yl)methylbenzoate 
• 107754-10-9 methyl 4-(5-amino-indol-3-ylmethyl)-3-methoxybenzoate 

Relevant academic research and scientific papers

SUBSTITUTED INDOLES

Disclosed herein are substituted indole cysteinyl leukotriene receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

A study of 5-nitroindole alkylation

A detailed study of the 5-nitroindole alkylation, the key step in the synthesis of Zafirlukast, is presented. A broad distribution of alkyl derivatives has been found. 2,3- And 1,3-dialkylindoles can be selectively obtained in a ZnBr2-catalyzed

Investigation into the acidification process of zafirluskast nitroacid leads to a surprising improvement in product quality

An investigation into the acidification step of the zafirlukast nitroacid process was conducted by varying a range of parameters, including acid molarity, addition time, final pH, and temperature. A significant and unexpected improvement in product quality was achieved by using dilute rather than concentrated acid, independent of the final pH, and without a reduction in yield. The change to the dilute-acid process could be accommodated within the constraints of the existing registered process.

A general method for C3 reductive alkylation of indoles

General indole C3 reductive alkylation conditions have been developed. The scope of this reaction includes C2 unsubstituted indoles, aryl and alkyl aldehydes, as well as N-H and N-alkyl indole substrates.

Bicyclic carbamates and methods of treating inflammatory diseases using the same

A compound of the formula STR1 wherein R is defined herein is useful as an anti-inflammatory agent.

Evolution of a series of peptidoleukotriene antagonists: Synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles

1,3,5-Substituted indoles and indazoles have been studied as receptor antagonists of the peptidoleukotrienes. The best of these compounds generally had a methyl group at the N1 position, a [(cyclopentyloxy)carbonyl]amino or 2-cyclopentylacetamido or N'-cyclopentylureido group at the C-5 position, and an arysulfonyl amide group as part of the acidic chain at the C-3 position of the ring. Such compounds had in vitro dissociation constants K(B) in the range 10-9-10-11 M on guinea pig trachea against LTE4 as agonist and inhibition constants (K(i)) ≤ 10-9 M on guinea pig parenchymal membranes against [3H]LTD4. A number of compounds were orally effective at doses ≤1 mg/kg in blocking LTD4-induced 'dyspnea' in guinea pigs. Compound 45 [N-[4-[[5-[[cyclopentyloxy)carbonyl]amino]-1-methylindol-3-yl]methyl]- 3-methoxybenzoyl]-2-methyl]benzenesulfonamide, ICI 204,219; pK(B) = 9.67 ± 0.13, K(i) = 0.3 ± 0.03 nM, po ED50 = 0.3 mg/kg] is currently under clinical investigation for asthma. In the indole series, certain alkylsulfonyl amides possessing a 3-cyanobenzyl substituent at the N-1 position (60, 61) were produced that had K(B) ≤ 10-9 M on guinea pig trachea.

Indole and indazole keto sulphones as leukotriene antagonists

This invention provides a series of novel keto sulfones of formula I STR1 in which the group =A-- is selected from =C(Ra)-- and =N-- and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Heterocyclic amide derivatives and pharmaceutical use

The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R1, R2, L, X, Y, Z, A1, Q, A2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process. STR1