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Although such complex structures are challenging targets in synthetic organic chemistry, efficient synthetic approaches will open a new chemical space for pharmaceutical candidates. This review provides an account of our recent achievements in developing organocatalytic approaches to attractive molecular platforms based on optically active sp<jats:sup>3<\/jats:sup> carbons integrating four different functional groups. These methodologies include asymmetric cycloetherification and cyanation of multifunctional ketones, both of which take advantage of the mild characteristics of organocatalytic activation. Enzyme\u2010like but non\u2010enzymatic organocatalytic systems can be used to precisely manufacture molecules containing complex chiral structures without substrate specificity problems. In addition, these catalytic systems control not only stereoselectivity but also site\u2010selectivity and do not induce side reactions even from substrates with rich functionality.<\/jats:p>","DOI":"10.1002\/tcr.202200200","type":"journal-article","created":{"date-parts":[[2022,9,27]],"date-time":"2022-09-27T02:12:14Z","timestamp":1664244734000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Organocatalytic Access to Tetrasubstituted Chiral Carbons Integrating Functional Groups"],"prefix":"10.1002","volume":"23","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9272-2937","authenticated-orcid":false,"given":"Keisuke","family":"Asano","sequence":"first","affiliation":[{"name":"Institute for Catalysis Hokkaido University Sapporo  Hokkaido 001-0021 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