651729-70-3Relevant academic research and scientific papers
Intramolecular Oxidative Coupling between Unactivated Aliphatic C-H and Aryl C-H Bonds
Liao, Yang,Zhou, Yi,Zhang, Zhen,Fan, Junzhen,Liu, Feng,Shi, Zhangjie
supporting information, p. 1251 - 1257 (2021/03/03)
Direct oxidative coupling of different inert C-H bonds is the most straightforward and environmentally benign method to construct C-C bonds. In this paper, we developed a Pd-catalyzed intramolecular oxidative coupling between unactivated aliphatic and aryl C-H bonds. This chemistry showed great potential to build up fused cyclic scaffolds from linear substrates through oxidative couplings. Privileged chromane and tetralin scaffolds were constructed from readily available linear starting materials in the absence of any organohalides and organometallic partners.
Rapid Construction of Tetralin, Chromane, and Indane Motifs via Cyclative C-H/C-H Coupling: Four-Step Total Synthesis of (±)-Russujaponol F
Zhuang, Zhe,Herron, Alastair N.,Liu, Shuang,Yu, Jin-Quan
supporting information, p. 687 - 692 (2021/01/25)
The development of practical C-H/C-H coupling reactions remains a challenging yet appealing synthetic venture because it circumvents the need to prefunctionalize both coupling partners for the generation of C-C bonds. Herein we report a cyclative C(sp3)-H/C(sp2)-H coupling reaction of free aliphatic acids enabled by a cyclopentane-based mono-N-protected β-amino acid ligand. This reaction uses inexpensive sodium percarbonate (Na2CO3·1.5H2O2) as the sole oxidant and generates water as the only byproduct. A range of biologically important scaffolds, including tetralins, chromanes, and indanes, can be easily prepared by this protocol. Finally, the synthetic application of this methodology is demonstrated by the concise total synthesis of (±)-russujaponol F in a four-step sequence starting from readily available phenylacetic acid and pivalic acid through sequential functionalizations of four C-H bonds.
PIPERIDINYL-3-(ARYLOXY)PROPANAMIDES AND PROPANOATES
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Paragraph 0179; 0202; 0207, (2019/09/18)
Disclosed are compounds of Formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6,R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.
Process for preparing isomerically pure prodrugs of proton pump inhibitors
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Page/Page column 18, (2010/02/10)
Synthetic methods for preparing isomerically pure N-arylsulfonyl derivatives of proton pump inhibitors which include a substituted benzimidazole nucleus are shown by the synthetic schemes and experimental description.
PRODRUGS OF PROTON PUMP INHIBITORS
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Page 184, (2010/02/06)
Prodrugs of proton pump inhibitors of Formulas 1 through 4, (I-IV), where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
