Since 2015, the sustainable development goals of the United Nations established a route map to achieve a sustainable society, pushing the industry to aim for sustainable processes. Biorefineries have been studied as the technological scheme to process integrally renewable resources. The so-called “bioactive” compounds (BACs) have been of high interest, given their high added value and potential application in pharmaceutics and health, among others. However, there are still elements to be addressed to consider them as economic drivers of sustainable processes. First, BACs can be produced from many sources and it is important to identify feedstocks for this purpose. Second, a sustainable production process should also consider valorizing the remaining components. Finally, feedstock availability plays an important role in affecting the process scale, logistics, and feasibility. This work consists of a review on the feedstocks for the sustainable production of BACs in biorefineries, covering the type of BAC, composition, and availability. Some example biorefineries are proposed using wheat straw, hemp and grapevine shoots. As a main conclusion, multiple raw materials have the potential to obtain BACs that can become economic drivers of biorefineries. This is an interesting outlook, as the integral use of the feedstocks may not only allow obtaining different types of BACs, but also other fiber products and energy for the process self-supply.