77093-97-1

Upstream product

• 67-56-1 methanol 
• 52727-44-3 2,3-dihydro-5H-oxazolo<2,3-b>quinazolin-5-one 
• 77189-70-9 2-<3-(2-cloroethyl)ureido>benzonitrile 
• 77093-92-6 methyl 2-<3-(2-chloroethyl)ureido>benzoate 
• 459836-89-6 2-amino-N-(2-methoxyethyl)benzamide 
• 118-48-9 isatoic anhydride 
• 109-85-3 2-methoxyethylamine 
• 6919-61-5 N-methoxy-N-methylbenzamide 
• 77093-94-8 2-(2-chloroethylamino)-4H-<3,1>benzoxazin-4-one hydrochloride 
• 13908-44-6 2-<3-(2-chloroethyl)ureido>benzoic acid 
• 118-92-3 anthranilic acid 
• 77093-93-7 2-(2-chloroethylamino)-4H-<3,1>benzoxazin-4-one 
• 1885-29-6 anthranilic acid nitrile 
• 5081-87-8 3-(2-chloroethyl)-2,4-dioxo-1,2,3,4-tetrahydroquinazoline 

Relevant academic research and scientific papers

1,3,4-OXADIAZOLE HOMOPHTHALIMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to novel compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a medicinal use thereof, and a method for preparing the same. The novel compounds according to the present invention, stereoisomers thereof or pharmaceutically acceptable salts thereof have the histone deacetylase 6 (HDAC6) inhibitory activity, and are effective in preventing or treating HDAC6-related diseases, comprising infectious diseases; neoplasm; endocrinopathy; nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; eye and ocular adnexal diseases; circulatory diseases; respiratory diseases; digestive diseases; skin and subcutaneous tissue diseases; musculoskeletal system and connective tissue diseases; and teratosis or deformities, or chromosomal aberration.

Iridium-Catalyzed C-H Amination of Weinreb Amides: A Facile Pathway toward Anilines and Quinazolin-2,4-diones

C-H amination of arenes directed by weakly coordinating Weinreb amides has been achieved with an iridium catalyst and 2,2,2-trichloroethoxycarbonyl (Troc) azide as an aminating agent, providing a robust method of producing synthetic useful ortho-TrocNH aryl Weinreb amides. Taking advantage of the reactivity of Weinreb amide and Troc groups in the amination products, selective hydrolysis was achieved as an attractive process for the synthesis of ortho-NH2 aryl Weinreb amides, which are the building blocks useful in the synthesis of bioactive compounds, and cascade aminocyclization with primary amines was successful and provided an efficient pathway for the construction of quinazolin-2,4-diones, which are present in various alkaloids and natural products.

Reactions of o-Aminonitriles with Isocyanates. 1. A Two-Step Synthesis of 2,6-Dihydroimidazoquinazolin-5-(3H)one

The reaction of anthranilonitrile with 2-chloroethyl isocyanate yields 2-benzonitrile (6) which, upon heating, or treatment with base, undergoes a double cyclization to form 2,6-dihydroimidazoquinazolin-5-(3H)one (8) in excellent yield.When heated with hydrochloric acid, 6 is converted initially into 2-(2-chloroethylamino)-4H-benzoxazin-4-one (18) and further into 3-(2-chloroethyl)-2,4-(1H,3H)quinazolinedione (15).The acid-catalyzed reaction of 2,3-dihydro-5H-oxazoloquinazolin-5-one (14) with nucleophilic reagents yields 3-substituted 2,4-(1H,3H)quinazolinediones.