270902-65-3

Upstream product

• 136289-11-7 (4R,4aS,7R,7aR)-4-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-7-methoxy-2,2-dimethyl-tetrahydro-6H-furo[3,2-d][1,3]dioxin-6-one 
• 6605-22-7 3,5:6,7-bis-O-(1-methylethylidene)-α-D-glucoheptonic γ-lactone 
• 1120352-71-7 D-glycero-D-gulco-hepteno-1,4-lactone 
• 89-67-8 α-D-glucoheptonic γ-lactone 

Downstream Products

• 958075-64-4 (2R,3R,4S,5R,6E)-7-cyclopentyl-3,4,5-trihydroxy-2-methoxy-N-[(3S)-2-oxo-7-phenyl-2,3,4,5-tetrahydro-1H-1-benzazepin-3-yl]hept-6-enamide 
• 958489-65-1 (3R,4R,5S)-4-hydroxy-5-[(1R,2E)-1-hydroxy-3-phenylprop-2-en-1-yl]-3-methoxydihydrofuran-2(3H)-one 
• 958489-61-7 (3R,4R,5S)-5-[(1R,2E)-3-(2-fluorophenyl)-1-hydroxyprop-2-en-1-yl]-4-hydroxy-3-methoxydihydrofuran-2(3H)-one 
• 958489-63-9 (3R,4R,5S)-5-[(1R,2E)-3-(4-fluorophenyl)-1-hydroxyprop-2-en-1-yl]-4-hydroxy-3-methoxydihydrofuran-2(3H)-one 
• 958489-59-3 (3R,4R,5S)-5-[(1R,2E)-3-cyclohexyl-1-hydroxyprop-2-en-1-yl]-4-hydroxy-3-methoxydihydrofuran-2(3H)-one 
• 958489-58-2 (2R,3R,4S,5R,6E)-7-cyclohexyl-3,4,5-trihydroxy-2-methoxy-N-[(3R)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl]hept-6-enamide 

Relevant academic research and scientific papers

Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators

To combat multidrug-resistant Gram-positive bacteria, new antimicrobials particularly those with novel mechanism of action are badly needed. Different with conventional antibiotics which are typical inhibitors, small-molecule activators of bacterial ClpP represent a new class of antibiotics. No ClpP activator has been developed for clinical trial. Herein, we conducted a screening on our library of bengamide-like ring-opened analogues and found that L472-2 possesses a low minimum inhibitory concentration (MIC) against S.aureus and shows no activity for ClpP activation in vitro, but it displayed reduced antibacterial activity against S. aureus with clpP deletion. In order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity, we perform further structural modifications starting from L472-2. Compound 37 remains the antimicrobial activity and activation of ClpP protein in vitro, which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.

CERTAIN SUBSTITUTED CAPROLACTAMS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN TREATING TUMORS

The present invention relates to certain substituted caprolactam compounds of formula (I), where R1 is (C1-6)alkyl or (C3-6)cycloalkyl; R2 is hydrogen or (C1-6)alkyl; X is (C1-12)alkylene; (C2-12)alkenylene; or (C2-12)alkynylene; m is 0 or 1; and R3 is (C

An Expedient Synthesis of LAF389, a Bengamide B Analogue

An optimized, convergent, safe synthesis of LAF389 (9), an anticancer agent analogous to bengamide B, is described. Starting from α-D- glucoheptonic (D-glycero-D-gulo-heptonic acid) γ-lactone (10), the lactone 15 was constructed in five steps. Major impro

Use of certain substituted caprolactams in treating tumors

The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Certain substituted caprolactam carbonates and ethers, pharmaceutical compositions containing them and their use in treating tumors

The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Total syntheses of bengamides B and E

Total syntheses of the cytotoxic marine natural products bengamides B and E are described. Both bengamides are prepared via amide coupling of a protected polyhydroxylated lactone intermediate 9 with a suitably substituted aminocaprolactam intermediate. Lactone 9 is prepared in five steps from commercially available α-D-glucoheptonic γ-lactone. The key reactions are a selective deprotection of a 1,2-acetonide in the presence of a 1,3-acetonide and an (E)-selective olefination of an unstable aldehyde using a gem-dichromium reagent. The bengamide B lactam intermediate 10 is prepared in seven steps from commercially available (5R)-5-hydroxy-L-lysine (12). The desired S-configuration at the γ-OH lactam position is established using the Mitsunobu reaction.

Use of certain substituted caprolactams in treating tumors

The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Certain substituted caprolactams, pharmaceutical compositions containing them and a process for their preparation

The present invention relates to certain substituted caprolactam compounds of formula (I), where R1is (C1-6)alkyl or (C3-6)cycloalkyl; R2hydrogen or (C1-6)alkyl; X is (C1-12)alkynylene; (C