Iridium-catalysed C-H borylation of β-aryl-aminopropionic acids
Iridium-catalysed catalytic, regioselective C-H borylation of β-aryl-aminopropionic acid derivatives gives access to 3,5-functionalised protected β-aryl-aminopropionic acid boronates. The synthetic versatility of these new boronates is demonstrated through sequential one-pot functionalisation reactions to give diverse building blocks for medicinal chemistry. The C-H borylation is also effective for dipeptide substrates. We have exemplified this methodology in the synthesis of a pan αv integrin antagonist.
MacDonald, Simon J. F.,Nortcliffe, Andrew,Robinson, Henry,Simelis, Klemensas,Stillibrand, Joe
supporting information
p. 6696 - 6701
(2020/09/21)
SUBSTITUTED BENZIMIDAZOLES AS POTASSIUM CHANNEL INHIBITORS
The present invention relates to a compound of the general formula (I). The compounds of formula I are useful for treatment of a cardiac disease, disorder or condition in a mammal.
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Page/Page column 65; 66
(2019/03/05)
BENZIMIDAZOLE DERIVATIVES USEFUL AS POTASSIUM CHANNEL INHIBITORS
The present invention relates to compounds of the general formula (I). The compounds of formula I are potassium channel inhibitors useful for treatment of a cardiac disease, disorder or condition in a mammal.
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Page/Page column 61
(2019/03/12)
Novel efficient method for synthesizing chiral beta-amino acid
The invention relates to a synthesis method of a compound as shown by the formula (I), namely chiral beta-amino acid: an aromatic aldehyde compound. An aromatic aldehyde compound and a chiral amine auxiliary form Schiff base, and then the Schiff base is r
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Paragraph 0065; 0067; 0069; 0079; 0080; 0081
(2019/01/08)
Microwave Assisted Synthesis of Trifluoro Substituted 2-Aminobenzimidazole Derivatives via Iodoacetic Acid Mediated One-pot Condensation
Microwave-assisted efficient one-pot syntheses of trifluoro substituted 2-aminobenzimidazole derivative were synthesized using iodoacetic acid mediated cyclodesulfurization of thioureas. This method eliminates need to handle preformed substituted thioureas, requires lesser reaction time and temperature, is facile, and also gives higher yields of the target molecules.
Sriram,Sapthagiri,Ilavarasan,Ravi
p. 2440 - 2446
(2017/07/25)
NOVEL POTASSIUM CHANNEL INHIBITORS
The present invention relates to a compound of the general formula (I). The compounds of formula (I) are useful for treatment of a cardiac disease, disorder or condition in a mammal.
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Page/Page column 65
(2017/09/15)
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