摘要:
The present invention relates to a process for the preparation of amides, comprising reacting amines with carboxylic acids in the presence of silicon amines. The present invention further relates to a process for the preparation of quinazoline derivatives, comprising reacting amines with carboxylic acids in the presence of silicon amines to obtain amides and contacting the resultant amides with quinazoline.
摘要:
The present invention provides a process for preparing an amide, which comprises reacting an amine with an ester in a molten form in the absence of a solvent.
摘要:
A compound of formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' are independently the same or different and each represent hydrogen, hydroxy, or lower alkoxy, or any vicinal two of R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' combined together represent --O--(CH.sub.2).sub.n --O--, wherein n=1 or 2; R.sub.4 represents methylene or halomethyl; and X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are independently the same or different and each represent hydrogen or halogen; or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition that contains an effective amount of a compound of formula I together with a pharmaceutically acceptable excipient, and a method of treating cancer that involves the administration of an effective amount of the compound of formula I to a patient in need thereof.
摘要:
A series of novel polyamine-linked acridine dimers and derivatives thereof are described. The polyamine-linked acridine dimers and derivatives are potential anti-cancer agents.
摘要:
A process of preparing 2-cyano-3,5-dimethyl-4-methoxypyridine. The process includes the steps of: acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-carboxamido-3,5-dimethyl-4(1H)-pyridone; methylating 2-carboxamido-3,5-dimethyl-4(1H)-pyridone to obtain 2-carboxamido-3,5-dimethyl-4-methoxypyridine; and dehydrating said 2-carboxamido-3,5-dimethyl-4-methoxypyridone to obtain 2-cyano-3,5-dimethyl-4-methoxypyridine.
摘要:
A process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine including the steps of acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone; halogenating 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone to obtain 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine; methoxylating 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine to obtain 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine; and reducing 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine to obtain 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine.
摘要:
An aqueous inhalation pharmaceutical composition comprising a polypeptide or protein is provided. The composition of the present invention can improve the bioavailability of the polypeptide and protein, and avoid inducing toxicity in the lung.
摘要:
A new method for the preparation of chiral 4-substituted 2-piperidinones, trans-3,4-disubstituted 2-piperidinones, and trans-3,4-disubstituted piperidines is invented. Chiral paroxetine can be obtained from a chiral trans-3,4-disubstituted piperidine intermediate in high purity and good selectivity.
摘要:
An aqueous inhalation pharmaceutical composition comprising a polypeptide or protein is provided. The composition of the present invention can improve the bioavailability of the polypeptide and protein, and avoid inducing toxicity in the lung.
摘要:
A method for synthesis of C2-symmetric diamino diol mediated by titanium complexes is provided. A substituted-L-phenylalaninal undergoes pinacol coupling to yield the corresponding C2-symmetric (1S,2R,3R,4S)-1,4-diamino 2,3-diol in the presence of Cp2TiCl2/ZnCl2 and zinc metal, mediated in good yield and highly selective. This titanium-catalyzed reaction yields diaminodiol, offering a convenient alternative method to the synthesis of C2-symmetric peptidic protease inhibitors. Consequently, the method allows to synthesize TL-3 via titanium complex in moderate yield.