Herein we report new cascade processes for the easy access to 1-substituted and C-unsubstituted 3-isoquinolinones. The Mannich initiated cascade reaction led to the synthesis of novel 1-substituted 3-isoquinolinones under catalyst-free conditions in the presence of nitromethane and dimethylmalonate as nucleophiles without the use of any solvent. The optimization of the synthesis of the starting material in a more environmentally benign manner, allowed the identification of a common intermediate useful for the synthesis of C-unsubstituted 3-isoquinolinones as well. The synthetic utility of 1-substituted 3-isoquinolinones was also demonstrated.

A facile access to 1-substituted and unsubstituted 3-isoquinolinones via Mannich or Sn2 initiated cascade reactions under catalyst-free conditions

A fast, high-yield one-step reaction is proposed for conjugating an MRI contrast agent to carboxylic acids and is demonstrated for synthesizing a blood-pool contrast agent that reversibly binds to albumin for in vivo vascular MRI. 

Efficient one-step amide formation using amino porphyrins

Amide is a fundamental group that is present in molecular structures of all domains of organic chemistry and the construction of this motif with high atom economy is the focus of the current research. Specifically, N-methyl amides are valuable building blocks in natural products and pharmaceutical science. Due to the volatile nature of methyl amine, the generation of N-methyl amides using simple acids with high atom economy is rare. Herein, we disclose an atom economic protocol to prepare this valuable motif under DABCO/Fe3O4 cooperative catalysis. This protocol is operationally simple and compatible with a range of aliphatic and (hetero)aromatic acids with very good yields (60–99%). Moreover, the Fe3O4 can be easily recovered and high efficiency is maintained for up to ten cycles.

/pdf/catalytic-n-methyl-amidation-of-carboxylic-acids-under-26n3orsv.pdf

Catalytic N-methyl amidation of carboxylic acids under cooperative conditions

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Catalytic N-methyl amidation of carboxylic acids under cooperative conditions