47 results about "Butenamide" patented technology

The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.

The present invention relates to an improved process for the preparation of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethyl amino)-(2E)-2-butenamide (2Z)-2-butenedioate (1:2) represented by the following structural formula:

The invention discloses a simple and efficient method for synthesizing 4-arylbutyric acid derivatives. Removable 8-aminoquinoline is used as a guiding group to control the regioselectivity of the reaction, and non-activated 3-butenamide is used. As a reaction raw material, it reacts with cheap, readily available, stable and efficient aryltrimethoxysilane to prepare and synthesize a series of functionalized 4-arylbutyric acid derivatives concisely and efficiently. The method has the advantages of simple operation, simple and easy-to-obtain reaction raw materials, easy separation and purification of products, high product yield and good reaction zone selectivity. The invention can provide related products for treating urea cycle disorder, novel anti-type II diabetes drugs, angiotensin-converting enzyme inhibitors and the like, and has good market potential and application value.

The invention discloses a method for synthesizing chlorambucil, which relates to the technical field of organic chemistry, and comprises the following steps: S1, the proportion content is 10.83%: 10.83% - 32.50%: 0.22% - 2.17%: 0.43% - 2.17%: 10.83%-54.17%: 10.83%-54.17% of 4-bromo-N,N-bis(2-chloroethyl)aniline, N-(quinolin-8-yl)but-3-enamide, Add the mixture made of palladium chloride, tri-n-butylphosphine tetrafluoroborate, potassium carbonate, benzoic acid and dimethyl sulfoxide in a molar volume ratio of 0.1mmol: 2mL to the reaction vessel and mix well; S2. The reaction vessel was placed in an oil bath at 135-145° C. and stirred vigorously for 24 hours. The present invention controls the region and chemoselectivity in the reaction by designing 8-aminoquinoline as a compound with a leaving group through a coupling reaction, effectively solving the problem of too many steps in the synthesis process of the existing chlorambucil problem, and the present invention has the characteristics of high reaction regioselectivity and yield, mild reaction conditions, and simple reaction and post-treatment purification process.

Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.

The present application relates to maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)aniline]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, crystalline forms thereof, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.