- Design and synthesis of new 4-alkylthio monocyclic β-lactams
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New types of monocyclic β-lactams constitute an important class of compounds due to their unique structures and natures. Here, the design and synthesis of new 4-alkylthio monocyclic β-lactams 2a and 3a are reported. Significantly, compounds 2a and 3a, while keeping a monocyclic system, were designed to contain all of the substructures provided by the cleavage of C(2)-C(3) bond in penicillins. Efficient synthetic pathways for compounds 2a and 3a were established based on two different strategies. Compound 2a was synthesized from raw materials, using 4-acetoxyazetidin-2-one as a key intermediate, through a ten-step synthetic sequence in 3% overall yield. Compound 3a was synthesized from potassium salt of penicillin G (17), using the degraded product 20 as a key intermediate, through a six-step synthetic sequence in 11% overall yield. 4-Alkylthioazetidin- 2-one derivatives, introduced in this study, could serve as valuable intermediates for the development of new monocyclic β-lactams.
- Lee, Sang Hyup
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p. 121 - 127
(2013/08/24)
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- Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
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The present application describes modulators of MCP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, n, R1, R2, R3, R4, R5, R10, R
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Page/Page column 22
(2010/02/14)
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- Process for producing arylsulfenyl halide
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A process for producing a compound of the formula (II): wherein Hal1 represents halogen and R1 and R2 each independently represents halogen, alkyl, alkoxy, nitro or cyano, which comprises allowing a halogenating agent to react with a compound of the formula (I): wherein Alk represents branched alkyl and R1 and R2 are as defined above.
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Page/Page column 7
(2010/11/29)
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