Artemisinin, a natural sesquiterpene isolated from the Artemisia annua L. plant, represents a remarkable achievement in the treatment against malaria. Since its discovery in the 1970’s, researchers readily started synthesizing this complex natural product containing an unusual endoperoxide fragment. Despite various total syntheses reported, only in the last decade the production jumped from extraction/bench scale to industrial manufacturing. In this sense, the objective of this contribution is to highlight the discovery, the most representative works towards the synthesis of artemisinin and its main derivatives used worldwide against malaria, and the path to the industrial production of these compounds.

Leprosy is an ancient infectious disease caused by Mycobacterium leprae. According to comparative genomics studies, this disease originated in Eastern Africa or the Near East and spread with successive human migrations. The Europeans and North Africans introduced leprosy into West Africa and the Americas within the past 500 years. In Brazil, this disease arrived with the colonizers who disembarked at the first colonies, Rio de Janeiro, Salvador and Recife, at the end of the sixteenth century, after which it was spread to the other states. In 1854, the first leprosy cases were identified in State of Amazonas in the north of Brazil. The increasing number of leprosy cases and the need for treatment and disease control led to the creation of places to isolate patients, known as leprosaria. One of them, Colonia Antônio Aleixo was built in Amazonas in 1956 according to the most advanced recommendations for isolation at that time and was deactivated in 1979. The history of the Alfredo da Matta Center (AMC), which was the first leprosy dispensary created in 1955, parallels the history of leprosy in the state. Over the years, the AMC has become one of the best training centers for leprosy, general dermatology and sexually transmitted diseases in Brazil. In addition to being responsible for leprosy control programs in the state, the AMC has carried out training programs on leprosy diagnosis and treatment for health professionals in Manaus and other municipalities of the state, aiming to increase the coverage of leprosy control activities. This paper provides a historical overview of leprosy in State of Amazonas, which is an endemic state in Brazil.

Neste trabalho, uma síntese curta e eficiente para o CMI-977 (LDP-977), um potente agente antiasmático oralmente ativo, é descrita. As etapas chave envolveram uma ciclização oxidativa de Mukaiyama, fornecendo a unidade trans-THF (tetrahidrofurano) e uma reação de homologação de Seyferth-Gilbert para construção da tripla ligação da molécula alvo. A síntese do bloco de construção chiral chave foi realizada a partir do emprego da resolução cinética hidrolítica de Jacobsen.

A short and efficient stereoselective total synthesis of CMI-977 (LDP-977), a potent and orally active anti-asthmatic compound, was developed. The key steps involve a highly diastereoselective Mukaiyama oxidative cyclization, which provides the trans-THF (tetrahydrofuran) unit and a Seyferth-Gilbert homologation to construct the triple bond in the target molecule. The synthesis of the key chiral building block was performed using Jacobsen hydrolytic kinetic resolution.