138459-91-3

Usage

Uses

thiazolidin e thione pharmaceutical intermediate

Upstream product

• 134469-06-0 thiazolidine-2-thione 
• 3282-30-2 pivaloyl chloride 
• 71591-75-8 sodium 2-mercaptothiazolinate 
• 96-53-7 2-mercaptothiazoline 
• 75-98-9 Trimethylacetic acid 
• 60-29-7 diethyl ether 

Downstream Products

• 141923-61-7 4-(2-hydroxyethyl)phenyl pivalate 
• 141923-60-6 2-(4-hydroxyphenyl)ethyl pivalate 
• 138488-63-8 2-(2-hydroxyphenyl)ethyl pivalate 
• 141923-58-2 2,2-Dimethyl-propionic acid 2-(2-hydroxy-ethyl)-cyclohexyl ester 
• 141923-57-1 2,2-Dimethyl-propionic acid 2-(2-hydroxy-cyclohexyl)-ethyl ester 
• 141923-59-3 2,2-Dimethyl-propionic acid 2-[2-(2,2-dimethyl-propionyloxy)-ethyl]-cyclohexyl ester 
• 17094-34-7 ethyl pivaloylacetate 
• 5434-57-1 n-Hexyl pivalate 
• 173034-99-6 4-((trimethylacetyl)oxy)aniline 
• 74052-89-4 N-(4-hydroxyphenyl)-2,2-dimethylpropanamide 
• 180713-54-6 3-methoxy-4-(pivaloyloxy)benzyl alcohol 

Relevant academic research and scientific papers

NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES

The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.

NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES

The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.

2-Chloro-1,3-dimethylimidazolinium chloride. 1. A powerful dehydrating equivalent to DCC

2-Chloro-1,3-dimethylimidazolinium chloride (DMC) (3) can act as a powerful dehydrating agent, replacing DCC (1) under nearly neutral conditions. Its application to acylation and dehydration is described.

Twisted amides as selective acylating agents for hydroxyl groups under neutral conditions: Models for activated peptides during enzymatic acyl transfer reaction

The highly twisted amide 2 served as a selective acylating agent for diols under neutral conditions. The reaction of primary-secondary diols with 2 led to the corresponding primary alkyl monopivalates. For diols containing alcoholic and phenolic hydroxyl groups, alcoholic hydroxyl groups were selectively acylated under neutral conditions, whereas, the opposite selectivity was observed under basic conditions, similar to the cases using acyl halides or acid anhydrides. Although 1 and 3 were unreactive to alcohols, 5-10 having substituent groups at C-4 were reactive to alcohols to give the corresponding acetates or benzoates.

Highly chemoselective acylation of substituted aminophenols with 3-(trimethylacetyl)-1,3-thiazolidine-2-thione

A general procedure for chemoselective acylation of substituted aminophenols has been developed. The N-acetylated products 7 and 10a-h were prepared by treating the aminophenols with 3-(trimethylacetyl)-1,3-thiazolidine-2-thione (1) in refluxing THF in 70-100% yield. The esters 8 and 13d,b,j of 3- and 4-amino phenols could be obtained in 70-94% yield by treating with NaH and 1.

Dynemicin analogs: syntheses, methods of preparation and use

A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Dynemicin analogs: synthesis, methods of preparation and use

A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Molecular design and chemical synthesis of potent enediynes. 2. Dynemicin model systems equipped with C-3 triggering devices and evidence for quinone methide formation in the mechanism of action of dynemicin A

Continuing the theme of the preceding article, this paper describes the synthesis and chemical properties of designed enediynes related to dynemicin A. These model systems are equipped with triggering devices at C-3 of the aromatic nucleus. The design of

Selective pivaloylation of hydroxyl groups by 3-Pivaloyl-1,3-thiazolidine-2-thione under neutral conditions

Under neutral conditions, 3-pivaloyl-l,3-thiazolidine-2-thione (PTT) was found to act as a selective pivaloylating reagent for hydroxyl groups. The primary hydroxyl groups of diols containing primary and secondary hydroxyl groups, and the phenolic hydroxyl groups of the diols having alcoholic and phenolic hydroxyl groups were selectively pivaloylated by PTT.