93853-60-2

Upstream product

• 154698-92-7 methyl 2-((tert-butyl(diphenyl)silyl)oxy)acetate 
• 58479-61-1 tert-butylchlorodiphenylsilane 
• 76271-74-4 2-((t-butyldiphenylsilyl)oxy)acetic acid 

Downstream Products

• 98525-49-6 {(2R,3S)-3-[(R)-1-(tert-Butyl-dimethyl-silanyloxy)-ethyl]-2-[2-(tert-butyl-diphenyl-silanyloxy)-acetylsulfanyl]-4-oxo-azetidin-1-yl}-oxo-acetic acid 2,2,2-trichloro-ethyl ester 
• 1203458-98-3 C₂₆H₃₁Cl₃N₂O₇Si 
• 1400585-43-4 (S)-N-(2-tert-butyldiphenylsilyloxyacetyl)-4-isopropyl-1,3-thiazolidine-2-thione 
• 274908-66-6 Ethyl (Z)-4-[tert-Butyl(diphenyl)siloxy]-3-oxobutanoate 
• 105455-35-4 2-{(2R,3R)-3-[(R)-1-(tert-Butyl-dimethyl-silanyloxy)-ethyl]-2-[2-(tert-butyl-diphenyl-silanyloxy)-acetylsulfanyl]-4-oxo-azetidin-1-yl}-3-methyl-but-2-enoic acid 2,2,2-trichloro-ethyl ester 
• 129573-93-9 2-{(2R,3S)-3-Bromo-2-[2-(tert-butyl-diphenyl-silanyloxy)-acetylsulfanyl]-4-oxo-3-[(R)-1-(2,2,2-trichloro-ethoxycarbonyloxy)-ethyl]-azetidin-1-yl}-3-methyl-but-2-enoic acid 2,2,2-trichloro-ethyl ester 

Relevant academic research and scientific papers

Direct anti Glycolate Aldol Reaction of Protected Chiral N-Hydroxyacetyl Thiazolidinethiones with Acetals Catalyzed by a Nickel(II) Complex

The direct and stereocontrolled addition of (S)-4-isopropyl-N-(2-pivaloyloxyacetyl)-1,3-thiazolidine-2-thione to dialkyl acetals of aromatic and α,β-unsaturated aldehydes catalyzed by 2.5–5 mol-% of a nickel(II) complex permits the synthesis of diastereom

FUSED 1,4-OXAZEPINES AS BET PROTEIN DEGRADERS

The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provids compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Proteins of the bromodomain and extra-terminal (BET) family are epigenetics "readers" and promising therapeutic targets for cancer and other human diseases. We describe herein a structure-guided design of [1,4]oxazepines as a new class of BET inhibitors and our subsequent design, synthesis, and evaluation of proteolysis-targeting chimeric (PROTAC) small-molecule BET degraders. Our efforts have led to the discovery of extremely potent BET degraders, exemplified by QCA570, which effectively induces degradation of BET proteins and inhibits cell growth in human acute leukemia cell lines even at low picomolar concentrations. QCA570 achieves complete and durable tumor regression in leukemia xenograft models in mice at well-tolerated dose-schedules. QCA570 is the most potent and efficacious BET degrader reported to date.

Total synthesis of piperazimycin a: a cytotoxic cyclic hexadepsipeptide

Pied piper: The first total synthesis of the title compound 1, a potent cytotoxic natural product has been achieved. The key elements include an efficient synthesis of the difficult-to-install (R,S)-gCIPip/ (S, S)-gOH Pip dipeptide fragment as well as mac

Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors

The present invention provides a compound of formula (1) wherein R1-R5, R25, R26, Y and X2 are defined as in claim 1. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and arc useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.