30877-30-6

Upstream product

• 858244-30-1 N-(2,4,5-trimethylphenyl)formamide 
• 75934-35-9 N-(2,2-Diethoxy-ethyl)-N-(3,4-dimethyl-phenyl)-2,2,2-trifluoro-acetamide 
• 75934-27-9 (2,2-Diethoxy-ethyl)-(3,4-dimethyl-phenyl)-amine 
• 407-25-0 trifluoroacetic anhydride 
• 791609-49-9 5,6-dimethyl-2,3-dihydro-1H-indole 
• 95-64-7 4-amino-o-xylene 
• 610-91-3 5-nitropseudocumene 
• 1188-33-6 N,N-dimethylformamide diethyl diacetal 

Downstream Products

• 791609-47-7 1-(5-O-triphenylmethyl-2,3-O-isopropylidene-α-D-ribofuranosyl) 5,6-dimethylindoline 
• 1538596-12-1 (5,6-dimethyl-1H-indol-3-yl)(phenyl)methanone 
• 791609-51-3 1-((3aR,4S,6R,6aR)-2,2-Dimethyl-6-trityloxymethyl-tetrahydro-furo[3,4-d][1,3]dioxol-4-yl)-5,6-dimethyl-1H-indole 

Relevant academic research and scientific papers

REV-ERB AGONISTS FOR THE TREATMENT OF TH17-MEDIATED INFLAMMATORY DISORDERS

The present disclosure provides compounds of Formula IA and Formula IB and their pharmaceutical compositions as selective agonists of REV-ERB-α: where R1, R2, R3, R4, R5, RX1, RX2, nA, nB, X, Y, and Z are described herein. The compounds are useful in various methods and uses, such as in the treatment of diseases including hyperglycemia, dyslipidemia, atherosclerosis, and autoimmune and inflammatory disorders or diseases, and as cancer therapeutics, such as for the treatment of glioblastoma, hepatocellular carcinoma, and colorectal cancer, and for immune-oncology purposes.

Regioselective glycosylation: Synthesis of α-indoline nucleosides

Novel indoline ribonucleosides with the α-N-glycoside configuration are synthesized with very high regioselectivity in 90-96% yield, using TMS protected indolines and 2,3-O-(1-methylethylidene)-5-O-(triphenylmethyl)- α/β-D-ribofuranose. The structures of

Low temperature dehydrogenation of α-indoline nucleosides

A variety of α-indole nucleosides are easily prepared from α-indoline nucleosides in excellent yield and at moderate temperature using manganese dioxide and molecular sieves in benzene or methylene chloride.

SYNTHESIS OF INDOLES FROM N-(TRIFLUOROACETYL)-2-ANILINO ACETALS

N-(trifluoroacetyl)indoles (3) are produced in high yield from appropriately ring-substituted N-(trifluoroacetyl)-2-anilino acetals (2) in boiling trifluoroacetic acid containing excess trifluoroacetic anhydride.Mild saponification provides the free indoles nearly quantitatively.The scope of the reaction is discussed.The ring closure follows solvolytic substitution of a trifluoroacetoxy group for one of the ethoxy groups in 2.The method has been extended to cyclization of N-(trifluoroacetyl)-α-anilinoacetone in hot polyphosphoric acid followed by saponification to yield 3-methylindole.

Intermediates for indoles

Ortho-nitrotoluenes are condensed with formamide acetals to yield the corresponding otho-nitro-β-aminestyrenes which undergo cyclization upon reduction to yield indoles.